TY  - CONF
AU  - Živanović, Marija
AU  - Selaković, Milica
AU  - Selaković, Života
AU  - Pavić, Aleksandar
AU  - Grahovac, Jelena
AU  - Šolaja, Bogdan A.
AU  - Srdić-Rajić, Tatjana
PY  - 2022
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/5695
PB  - Elsevier
C3  - European Journal of Cancer
T1  - 322 (PB102) - Cationic amphiphilic drugs as potential anticancer therapy for PDAC
VL  - 174S1
IS  - PB102
SP  - S114
DO  - 10.1016/S0959-8049(22)01106-6
ER  - 

@conference{
author = "Živanović, Marija and Selaković, Milica and Selaković, Života and Pavić, Aleksandar and Grahovac, Jelena and Šolaja, Bogdan A. and Srdić-Rajić, Tatjana",
year = "2022",
publisher = "Elsevier",
journal = "European Journal of Cancer",
title = "322 (PB102) - Cationic amphiphilic drugs as potential anticancer therapy for PDAC",
volume = "174S1",
number = "PB102",
pages = "S114",
doi = "10.1016/S0959-8049(22)01106-6"
}

Živanović, M., Selaković, M., Selaković, Ž., Pavić, A., Grahovac, J., Šolaja, B. A.,& Srdić-Rajić, T.. (2022). 322 (PB102) - Cationic amphiphilic drugs as potential anticancer therapy for PDAC. in European Journal of Cancer
Elsevier., 174S1(PB102), S114.
https://doi.org/10.1016/S0959-8049(22)01106-6

Živanović M, Selaković M, Selaković Ž, Pavić A, Grahovac J, Šolaja BA, Srdić-Rajić T. 322 (PB102) - Cationic amphiphilic drugs as potential anticancer therapy for PDAC. in European Journal of Cancer. 2022;174S1(PB102):S114.
doi:10.1016/S0959-8049(22)01106-6 .

Živanović, Marija, Selaković, Milica, Selaković, Života, Pavić, Aleksandar, Grahovac, Jelena, Šolaja, Bogdan A., Srdić-Rajić, Tatjana, "322 (PB102) - Cationic amphiphilic drugs as potential anticancer therapy for PDAC" in European Journal of Cancer, 174S1, no. PB102 (2022):S114,
https://doi.org/10.1016/S0959-8049(22)01106-6 . .

TY  - JOUR
AU  - Radaković, Nataša
AU  - Nikolić, Andrea
AU  - Terzić-Jovanović, Nataša
AU  - Stojković, Pavle
AU  - Stanković, Nada
AU  - Šolaja, Bogdan A.
AU  - Opsenica, Igor
AU  - Pavić, Aleksandar
PY  - 2022
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/4877
AB  - Candida albicans remains the main causal agent of candidiasis, the most common fungal infection with disturbingly high mortality rates worldwide. The limited diversity and efficacy of clinical antifungal drugs, exacerbated by emerging drug resistance, have resulted in the failure of current antifungal therapies. This imposes an urgent demand for the development of innovative strategies for effective eradication of candidal infections. While the existing clinical drugs display fungicidal or fungistatic activity, the strategy specifically targeting C. albicans filamentation, as the most important virulence trait, represents an attractive approach for overcoming the drawbacks related to clinical antifungals. The results acquired in this study revealed the significant potential of 5-aminotetrazoles as a new class of effective and safe anti-virulence agents. Moreover, these novel agents were active when applied both alone and in combination with clinically approved polyenes. Complete prevention of C. albicans morphogenetic yeast-to-hyphae transition was achieved at doses as low as 1.3 μM under conditions mimicking various filamentation-responsive stimuli in the human body, while no cardio- or hepatotoxicity was observed at doses as high as 200 μM. The treatment of C. albicans-infected zebrafish embryos with nystatin alone had low efficacy, while the combination of nystatin and selected 5-aminotetrazoles prevented fungal filamentation, successfully eliminating the infection and rescuing the infected embryos from lethal disseminated candidiasis. In addition, the most potent anti-virulence 5-aminotetrazole prevented C. albicans in developing the resistance to nystatin when applied in combination, keeping the fungus sensitive to the antifungal drug.
PB  - Elsevier
T2  - European Journal of Medicinal Chemistry
T1  - Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis
VL  - 230
SP  - 114137
DO  - 10.1016/j.ejmech.2022.114137
ER  - 

@article{
author = "Radaković, Nataša and Nikolić, Andrea and Terzić-Jovanović, Nataša and Stojković, Pavle and Stanković, Nada and Šolaja, Bogdan A. and Opsenica, Igor and Pavić, Aleksandar",
year = "2022",
abstract = "Candida albicans remains the main causal agent of candidiasis, the most common fungal infection with disturbingly high mortality rates worldwide. The limited diversity and efficacy of clinical antifungal drugs, exacerbated by emerging drug resistance, have resulted in the failure of current antifungal therapies. This imposes an urgent demand for the development of innovative strategies for effective eradication of candidal infections. While the existing clinical drugs display fungicidal or fungistatic activity, the strategy specifically targeting C. albicans filamentation, as the most important virulence trait, represents an attractive approach for overcoming the drawbacks related to clinical antifungals. The results acquired in this study revealed the significant potential of 5-aminotetrazoles as a new class of effective and safe anti-virulence agents. Moreover, these novel agents were active when applied both alone and in combination with clinically approved polyenes. Complete prevention of C. albicans morphogenetic yeast-to-hyphae transition was achieved at doses as low as 1.3 μM under conditions mimicking various filamentation-responsive stimuli in the human body, while no cardio- or hepatotoxicity was observed at doses as high as 200 μM. The treatment of C. albicans-infected zebrafish embryos with nystatin alone had low efficacy, while the combination of nystatin and selected 5-aminotetrazoles prevented fungal filamentation, successfully eliminating the infection and rescuing the infected embryos from lethal disseminated candidiasis. In addition, the most potent anti-virulence 5-aminotetrazole prevented C. albicans in developing the resistance to nystatin when applied in combination, keeping the fungus sensitive to the antifungal drug.",
publisher = "Elsevier",
journal = "European Journal of Medicinal Chemistry",
title = "Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis",
volume = "230",
pages = "114137",
doi = "10.1016/j.ejmech.2022.114137"
}

Radaković, N., Nikolić, A., Terzić-Jovanović, N., Stojković, P., Stanković, N., Šolaja, B. A., Opsenica, I.,& Pavić, A.. (2022). Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis. in European Journal of Medicinal Chemistry
Elsevier., 230, 114137.
https://doi.org/10.1016/j.ejmech.2022.114137

Radaković N, Nikolić A, Terzić-Jovanović N, Stojković P, Stanković N, Šolaja BA, Opsenica I, Pavić A. Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis. in European Journal of Medicinal Chemistry. 2022;230:114137.
doi:10.1016/j.ejmech.2022.114137 .

Radaković, Nataša, Nikolić, Andrea, Terzić-Jovanović, Nataša, Stojković, Pavle, Stanković, Nada, Šolaja, Bogdan A., Opsenica, Igor, Pavić, Aleksandar, "Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis" in European Journal of Medicinal Chemistry, 230 (2022):114137,
https://doi.org/10.1016/j.ejmech.2022.114137 . .

TY  - DATA
AU  - Radaković, Nataša
AU  - Nikolić, Andrea
AU  - Terzić-Jovanović, Nataša
AU  - Stojković, Pavle
AU  - Stanković, Nada
AU  - Šolaja, Bogdan A.
AU  - Opsenica, Igor
AU  - Pavić, Aleksandar
PY  - 2022
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/4878
PB  - Elsevier
T2  - European Journal of Medicinal Chemistry
T1  - Supplementary data for article: Radakovic, N.; Nikolić, A.; Jovanović, N. T.; Stojković, P.; Stankovic, N.; Šolaja, B.; Opsenica, I.; Pavic, A. Unraveling the Anti-Virulence Potential and Antifungal Efficacy of 5-Aminotetrazoles Using the Zebrafish Model of Disseminated Candidiasis. European Journal of Medicinal Chemistry 2022, 230, 114137. https://doi.org/10.1016/j.ejmech.2022.114137.
UR  - https://hdl.handle.net/21.15107/rcub_cherry_4878
ER  - 

@misc{
author = "Radaković, Nataša and Nikolić, Andrea and Terzić-Jovanović, Nataša and Stojković, Pavle and Stanković, Nada and Šolaja, Bogdan A. and Opsenica, Igor and Pavić, Aleksandar",
year = "2022",
publisher = "Elsevier",
journal = "European Journal of Medicinal Chemistry",
title = "Supplementary data for article: Radakovic, N.; Nikolić, A.; Jovanović, N. T.; Stojković, P.; Stankovic, N.; Šolaja, B.; Opsenica, I.; Pavic, A. Unraveling the Anti-Virulence Potential and Antifungal Efficacy of 5-Aminotetrazoles Using the Zebrafish Model of Disseminated Candidiasis. European Journal of Medicinal Chemistry 2022, 230, 114137. https://doi.org/10.1016/j.ejmech.2022.114137.",
url = "https://hdl.handle.net/21.15107/rcub_cherry_4878"
}

Radaković, N., Nikolić, A., Terzić-Jovanović, N., Stojković, P., Stanković, N., Šolaja, B. A., Opsenica, I.,& Pavić, A.. (2022). Supplementary data for article: Radakovic, N.; Nikolić, A.; Jovanović, N. T.; Stojković, P.; Stankovic, N.; Šolaja, B.; Opsenica, I.; Pavic, A. Unraveling the Anti-Virulence Potential and Antifungal Efficacy of 5-Aminotetrazoles Using the Zebrafish Model of Disseminated Candidiasis. European Journal of Medicinal Chemistry 2022, 230, 114137. https://doi.org/10.1016/j.ejmech.2022.114137.. in European Journal of Medicinal Chemistry
Elsevier..
https://hdl.handle.net/21.15107/rcub_cherry_4878

Radaković N, Nikolić A, Terzić-Jovanović N, Stojković P, Stanković N, Šolaja BA, Opsenica I, Pavić A. Supplementary data for article: Radakovic, N.; Nikolić, A.; Jovanović, N. T.; Stojković, P.; Stankovic, N.; Šolaja, B.; Opsenica, I.; Pavic, A. Unraveling the Anti-Virulence Potential and Antifungal Efficacy of 5-Aminotetrazoles Using the Zebrafish Model of Disseminated Candidiasis. European Journal of Medicinal Chemistry 2022, 230, 114137. https://doi.org/10.1016/j.ejmech.2022.114137.. in European Journal of Medicinal Chemistry. 2022;.
https://hdl.handle.net/21.15107/rcub_cherry_4878 .

Radaković, Nataša, Nikolić, Andrea, Terzić-Jovanović, Nataša, Stojković, Pavle, Stanković, Nada, Šolaja, Bogdan A., Opsenica, Igor, Pavić, Aleksandar, "Supplementary data for article: Radakovic, N.; Nikolić, A.; Jovanović, N. T.; Stojković, P.; Stankovic, N.; Šolaja, B.; Opsenica, I.; Pavic, A. Unraveling the Anti-Virulence Potential and Antifungal Efficacy of 5-Aminotetrazoles Using the Zebrafish Model of Disseminated Candidiasis. European Journal of Medicinal Chemistry 2022, 230, 114137. https://doi.org/10.1016/j.ejmech.2022.114137." in European Journal of Medicinal Chemistry (2022),
https://hdl.handle.net/21.15107/rcub_cherry_4878 .

TY  - JOUR
AU  - Kop, Tatjana J.
AU  - Terzić-Jovanović, Nataša
AU  - Žižak, Željko
AU  - Šolaja, Bogdan A.
AU  - Milić, Dragana R.
PY  - 2022
UR  - https://pubs.rsc.org/en/content/articlelanding/2022/ra/d2ra03717c
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/5523
AB  - Iron salt-promoted reaction of estrone and its derivatives with              meta              -chloroperoxybenzoic acid was developed and epoxyquinols were further transformed. Most compounds showed              in vitro              antiproliferative activity.                      ,                           A new oxidant, containing              m              -chloroperoxybenzoic acid (MCPBA) and an iron salt, was developed and used for oxidation of steroidal phenols to a quinol/epoxyquinol mixture. Reaction was optimized for estrone, by varying initiators (Fe-salts), reaction temperature, time and mode of MCPBA application. A series of five more substrates (17β-estradiol and its hydrophobized derivatives) was subjected to the optimized oxidation, providing corresponding              p              -quinols and 4β,5β-epoxyquinols in good to moderate yields. The obtained epoxyquinols were additionally transformed by oxidation, as well as the acid-catalyzed oxirane opening. In a preliminary study of the antiproliferative activity against human cancer cell lines, all newly synthesized compounds expressed moderate to high activity.
PB  - Royal Society of Chemistry
T2  - RSC AdvancesRSC Adv.
T1  - Iron salt-promoted oxidation of steroidal phenols by m -chloroperbenzoic acid: a route to possible antitumor agents
VL  - 12
IS  - 32
SP  - 20649
EP  - 20655
DO  - 10.1039/D2RA03717C
ER  - 

@article{
author = "Kop, Tatjana J. and Terzić-Jovanović, Nataša and Žižak, Željko and Šolaja, Bogdan A. and Milić, Dragana R.",
year = "2022",
abstract = "Iron salt-promoted reaction of estrone and its derivatives with              meta              -chloroperoxybenzoic acid was developed and epoxyquinols were further transformed. Most compounds showed              in vitro              antiproliferative activity.                      ,                           A new oxidant, containing              m              -chloroperoxybenzoic acid (MCPBA) and an iron salt, was developed and used for oxidation of steroidal phenols to a quinol/epoxyquinol mixture. Reaction was optimized for estrone, by varying initiators (Fe-salts), reaction temperature, time and mode of MCPBA application. A series of five more substrates (17β-estradiol and its hydrophobized derivatives) was subjected to the optimized oxidation, providing corresponding              p              -quinols and 4β,5β-epoxyquinols in good to moderate yields. The obtained epoxyquinols were additionally transformed by oxidation, as well as the acid-catalyzed oxirane opening. In a preliminary study of the antiproliferative activity against human cancer cell lines, all newly synthesized compounds expressed moderate to high activity.",
publisher = "Royal Society of Chemistry",
journal = "RSC AdvancesRSC Adv.",
title = "Iron salt-promoted oxidation of steroidal phenols by m -chloroperbenzoic acid: a route to possible antitumor agents",
volume = "12",
number = "32",
pages = "20649-20655",
doi = "10.1039/D2RA03717C"
}

Kop, T. J., Terzić-Jovanović, N., Žižak, Ž., Šolaja, B. A.,& Milić, D. R.. (2022). Iron salt-promoted oxidation of steroidal phenols by m -chloroperbenzoic acid: a route to possible antitumor agents. in RSC AdvancesRSC Adv.
Royal Society of Chemistry., 12(32), 20649-20655.
https://doi.org/10.1039/D2RA03717C

Kop TJ, Terzić-Jovanović N, Žižak Ž, Šolaja BA, Milić DR. Iron salt-promoted oxidation of steroidal phenols by m -chloroperbenzoic acid: a route to possible antitumor agents. in RSC AdvancesRSC Adv.. 2022;12(32):20649-20655.
doi:10.1039/D2RA03717C .

Kop, Tatjana J., Terzić-Jovanović, Nataša, Žižak, Željko, Šolaja, Bogdan A., Milić, Dragana R., "Iron salt-promoted oxidation of steroidal phenols by m -chloroperbenzoic acid: a route to possible antitumor agents" in RSC AdvancesRSC Adv., 12, no. 32 (2022):20649-20655,
https://doi.org/10.1039/D2RA03717C . .

TY  - JOUR
AU  - Opsenica, Igor
AU  - Selaković, Milica
AU  - Tot, Mikloš
AU  - Verbić, Tatjana
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Đurković-Đaković, Olgica
AU  - Šolaja, Bogdan A.
PY  - 2021
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/4389
AB  - Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three aminoquinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Antimalarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured. © 2021 Serbian Chemical Society. All rights reserved.
PB  - Belgrade : Serbian Chemical Society
T2  - Journal of the Serbian Chemical Society
T1  - New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria
VL  - 86
IS  - 2
SP  - 115
EP  - 123
DO  - 10.2298/JSC201225005O
ER  - 

@article{
author = "Opsenica, Igor and Selaković, Milica and Tot, Mikloš and Verbić, Tatjana and Srbljanović, Jelena and Štajner, Tijana and Đurković-Đaković, Olgica and Šolaja, Bogdan A.",
year = "2021",
abstract = "Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three aminoquinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Antimalarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured. © 2021 Serbian Chemical Society. All rights reserved.",
publisher = "Belgrade : Serbian Chemical Society",
journal = "Journal of the Serbian Chemical Society",
title = "New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria",
volume = "86",
number = "2",
pages = "115-123",
doi = "10.2298/JSC201225005O"
}

Opsenica, I., Selaković, M., Tot, M., Verbić, T., Srbljanović, J., Štajner, T., Đurković-Đaković, O.,& Šolaja, B. A.. (2021). New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria. in Journal of the Serbian Chemical Society
Belgrade : Serbian Chemical Society., 86(2), 115-123.
https://doi.org/10.2298/JSC201225005O

Opsenica I, Selaković M, Tot M, Verbić T, Srbljanović J, Štajner T, Đurković-Đaković O, Šolaja BA. New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria. in Journal of the Serbian Chemical Society. 2021;86(2):115-123.
doi:10.2298/JSC201225005O .

Opsenica, Igor, Selaković, Milica, Tot, Mikloš, Verbić, Tatjana, Srbljanović, Jelena, Štajner, Tijana, Đurković-Đaković, Olgica, Šolaja, Bogdan A., "New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria" in Journal of the Serbian Chemical Society, 86, no. 2 (2021):115-123,
https://doi.org/10.2298/JSC201225005O . .

TY  - DATA
AU  - Opsenica, Igor
AU  - Selaković, Milica
AU  - Tot, Mikloš
AU  - Verbić, Tatjana
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Đurković-Đaković, Olgica
AU  - Šolaja, Bogdan A.
PY  - 2021
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/4392
PB  - Belgrade : Serbian Chemical Society
T2  - Journal of the Serbian Chemical Society
T1  - Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O
VL  - 86
IS  - 2
UR  - https://hdl.handle.net/21.15107/rcub_cherry_4392
ER  - 

@misc{
author = "Opsenica, Igor and Selaković, Milica and Tot, Mikloš and Verbić, Tatjana and Srbljanović, Jelena and Štajner, Tijana and Đurković-Đaković, Olgica and Šolaja, Bogdan A.",
year = "2021",
publisher = "Belgrade : Serbian Chemical Society",
journal = "Journal of the Serbian Chemical Society",
title = "Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O",
volume = "86",
number = "2",
url = "https://hdl.handle.net/21.15107/rcub_cherry_4392"
}

Opsenica, I., Selaković, M., Tot, M., Verbić, T., Srbljanović, J., Štajner, T., Đurković-Đaković, O.,& Šolaja, B. A.. (2021). Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O. in Journal of the Serbian Chemical Society
Belgrade : Serbian Chemical Society., 86(2).
https://hdl.handle.net/21.15107/rcub_cherry_4392

Opsenica I, Selaković M, Tot M, Verbić T, Srbljanović J, Štajner T, Đurković-Đaković O, Šolaja BA. Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O. in Journal of the Serbian Chemical Society. 2021;86(2).
https://hdl.handle.net/21.15107/rcub_cherry_4392 .

Opsenica, Igor, Selaković, Milica, Tot, Mikloš, Verbić, Tatjana, Srbljanović, Jelena, Štajner, Tijana, Đurković-Đaković, Olgica, Šolaja, Bogdan A., "Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O" in Journal of the Serbian Chemical Society, 86, no. 2 (2021),
https://hdl.handle.net/21.15107/rcub_cherry_4392 .

TY  - JOUR
AU  - Srbljanović, Jelena
AU  - Bobić, Branko
AU  - Štajner, Tijana
AU  - Uzelac, Aleksandra
AU  - Opsenica, Igor
AU  - Terzić-Jovanović, Nataša
AU  - Bauman, Neda
AU  - Šolaja, Bogdan A.
AU  - Đurković-Đaković, Olgica
PY  - 2020
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/4054
AB  - ObjectivesMalaria treatment is impeded by increasing resistance to conventional antimalarial drugs. Here we explored the activity of ten novel benzothiophene, thiophene and benzene aminoquinolines.MethodsIn vitro testing was performed by the lactate dehydrogenase assay in chloroquine (CQ)-sensitive Plasmodium falciparum strain 3D7 and CQ-resistant (CQR) P. falciparum strain Dd2. In vivo activity was evaluated by a modified Thompson test using C57BL/6 mice infected with Plasmodium berghei ANKA strain.ResultsNine of the ten compounds had a lower 50% inhibitory concentration (IC50) than CQ against the CQR strain Dd2. Five of these compounds that were available for in vivo evaluation were shown to be non-toxic. All five compounds administered at a dose of 160mg/kg/day for 3 days prolonged the survival of treated compared with untreated mice. Untreated control mice died by Day 7 with a mean parasitaemia of 15%. Among treated mice, a dichotomous outcome was observed, with a two-third majority of treated mice dying by Day 17 with a low mean parasitaemia of 5%, whilst one-third survived longer with a mean hyperparasitaemia of 70%; specifically, five of these mice survived a mean of 25 days, whilst two even survived past Day 31.ConclusionsThe significant antimalarial potential of this aminoquinoline series is illustrated by its excellent in vitro activity against the CQR P. falciparum strain and significant in vivo activity. Interestingly, compounds ClAQ7, ClAQ9 and ClAQ11 were able to confer resistance to cerebral malaria and afford a switch to hyperparasitaemia to mice prone to the neurological syndrome.
PB  - Elsevier
T2  - Journal of Global Antimicrobial Resistance
T2  - Journal of Global Antimicrobial Resistance
T1  - Aminoquinolines afford resistance to cerebral malaria in susceptible mice
VL  - 23
SP  - 20
EP  - 25
DO  - 10.1016/j.jgar.2020.07.027
ER  - 

@article{
author = "Srbljanović, Jelena and Bobić, Branko and Štajner, Tijana and Uzelac, Aleksandra and Opsenica, Igor and Terzić-Jovanović, Nataša and Bauman, Neda and Šolaja, Bogdan A. and Đurković-Đaković, Olgica",
year = "2020",
abstract = "ObjectivesMalaria treatment is impeded by increasing resistance to conventional antimalarial drugs. Here we explored the activity of ten novel benzothiophene, thiophene and benzene aminoquinolines.MethodsIn vitro testing was performed by the lactate dehydrogenase assay in chloroquine (CQ)-sensitive Plasmodium falciparum strain 3D7 and CQ-resistant (CQR) P. falciparum strain Dd2. In vivo activity was evaluated by a modified Thompson test using C57BL/6 mice infected with Plasmodium berghei ANKA strain.ResultsNine of the ten compounds had a lower 50% inhibitory concentration (IC50) than CQ against the CQR strain Dd2. Five of these compounds that were available for in vivo evaluation were shown to be non-toxic. All five compounds administered at a dose of 160mg/kg/day for 3 days prolonged the survival of treated compared with untreated mice. Untreated control mice died by Day 7 with a mean parasitaemia of 15%. Among treated mice, a dichotomous outcome was observed, with a two-third majority of treated mice dying by Day 17 with a low mean parasitaemia of 5%, whilst one-third survived longer with a mean hyperparasitaemia of 70%; specifically, five of these mice survived a mean of 25 days, whilst two even survived past Day 31.ConclusionsThe significant antimalarial potential of this aminoquinoline series is illustrated by its excellent in vitro activity against the CQR P. falciparum strain and significant in vivo activity. Interestingly, compounds ClAQ7, ClAQ9 and ClAQ11 were able to confer resistance to cerebral malaria and afford a switch to hyperparasitaemia to mice prone to the neurological syndrome.",
publisher = "Elsevier",
journal = "Journal of Global Antimicrobial Resistance, Journal of Global Antimicrobial Resistance",
title = "Aminoquinolines afford resistance to cerebral malaria in susceptible mice",
volume = "23",
pages = "20-25",
doi = "10.1016/j.jgar.2020.07.027"
}

Srbljanović, J., Bobić, B., Štajner, T., Uzelac, A., Opsenica, I., Terzić-Jovanović, N., Bauman, N., Šolaja, B. A.,& Đurković-Đaković, O.. (2020). Aminoquinolines afford resistance to cerebral malaria in susceptible mice. in Journal of Global Antimicrobial Resistance
Elsevier., 23, 20-25.
https://doi.org/10.1016/j.jgar.2020.07.027

Srbljanović J, Bobić B, Štajner T, Uzelac A, Opsenica I, Terzić-Jovanović N, Bauman N, Šolaja BA, Đurković-Đaković O. Aminoquinolines afford resistance to cerebral malaria in susceptible mice. in Journal of Global Antimicrobial Resistance. 2020;23:20-25.
doi:10.1016/j.jgar.2020.07.027 .

Srbljanović, Jelena, Bobić, Branko, Štajner, Tijana, Uzelac, Aleksandra, Opsenica, Igor, Terzić-Jovanović, Nataša, Bauman, Neda, Šolaja, Bogdan A., Đurković-Đaković, Olgica, "Aminoquinolines afford resistance to cerebral malaria in susceptible mice" in Journal of Global Antimicrobial Resistance, 23 (2020):20-25,
https://doi.org/10.1016/j.jgar.2020.07.027 . .

TY  - JOUR
AU  - Manzano, Jose Ignacio
AU  - Konstantinović, Jelena M.
AU  - Scaccabarozzi, Diletta
AU  - Perea, Ana
AU  - Pavić, Aleksandar
AU  - Cavicchini, Loredana
AU  - Basilico, Nicoletta
AU  - Gamarro, Francisco
AU  - Šolaja, Bogdan A.
PY  - 2019
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/3287
AB  - Among neglected tropical diseases, leishmaniasis is one of the most relevant with an estimated 30,000 deaths annually. Existing therapies have serious drawbacks in safety, drug resistance, field-adapted application and cost; therefore, new safer and shorter treatments are needed for this disease. Here we report on the synthesis of novel 4-amino-7-chloroquinoline-based compounds with leishmanicidal activity, together with deeper insight into the mechanism of action of our previously published hit compound 1. New derivatives showed comparable activity to 1 against both promastigote and intracellular amastigote forms of Leishmania infantum, with IC50 < 1 mM. Furthermore, we have determined that compound 1 induced a decrease of intracellular ATP levels, as well as a mitochondrial depolarization, together with an alteration of plasma membrane permeability and a significant ROS production. The inhibition of the energy metabolism of Leishmania plays an important role in the leishmanicidal mechanism of this compound. In all, these results support the consideration of compound 1 for the future development of new leishmanicidal drugs.
PB  - Elsevier
T2  - European Journal of Medicinal Chemistry
T1  - 4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania
VL  - 180
SP  - 28
EP  - 40
DO  - 10.1016/j.ejmech.2019.07.010
ER  - 

@article{
author = "Manzano, Jose Ignacio and Konstantinović, Jelena M. and Scaccabarozzi, Diletta and Perea, Ana and Pavić, Aleksandar and Cavicchini, Loredana and Basilico, Nicoletta and Gamarro, Francisco and Šolaja, Bogdan A.",
year = "2019",
abstract = "Among neglected tropical diseases, leishmaniasis is one of the most relevant with an estimated 30,000 deaths annually. Existing therapies have serious drawbacks in safety, drug resistance, field-adapted application and cost; therefore, new safer and shorter treatments are needed for this disease. Here we report on the synthesis of novel 4-amino-7-chloroquinoline-based compounds with leishmanicidal activity, together with deeper insight into the mechanism of action of our previously published hit compound 1. New derivatives showed comparable activity to 1 against both promastigote and intracellular amastigote forms of Leishmania infantum, with IC50 < 1 mM. Furthermore, we have determined that compound 1 induced a decrease of intracellular ATP levels, as well as a mitochondrial depolarization, together with an alteration of plasma membrane permeability and a significant ROS production. The inhibition of the energy metabolism of Leishmania plays an important role in the leishmanicidal mechanism of this compound. In all, these results support the consideration of compound 1 for the future development of new leishmanicidal drugs.",
publisher = "Elsevier",
journal = "European Journal of Medicinal Chemistry",
title = "4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania",
volume = "180",
pages = "28-40",
doi = "10.1016/j.ejmech.2019.07.010"
}

Manzano, J. I., Konstantinović, J. M., Scaccabarozzi, D., Perea, A., Pavić, A., Cavicchini, L., Basilico, N., Gamarro, F.,& Šolaja, B. A.. (2019). 4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania. in European Journal of Medicinal Chemistry
Elsevier., 180, 28-40.
https://doi.org/10.1016/j.ejmech.2019.07.010

Manzano JI, Konstantinović JM, Scaccabarozzi D, Perea A, Pavić A, Cavicchini L, Basilico N, Gamarro F, Šolaja BA. 4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania. in European Journal of Medicinal Chemistry. 2019;180:28-40.
doi:10.1016/j.ejmech.2019.07.010 .

Manzano, Jose Ignacio, Konstantinović, Jelena M., Scaccabarozzi, Diletta, Perea, Ana, Pavić, Aleksandar, Cavicchini, Loredana, Basilico, Nicoletta, Gamarro, Francisco, Šolaja, Bogdan A., "4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania" in European Journal of Medicinal Chemistry, 180 (2019):28-40,
https://doi.org/10.1016/j.ejmech.2019.07.010 . .

TY  - DATA
AU  - Manzano, Jose Ignacio
AU  - Konstantinović, Jelena M.
AU  - Scaccabarozzi, Diletta
AU  - Perea, Ana
AU  - Pavić, Aleksandar
AU  - Cavicchini, Loredana
AU  - Basilico, Nicoletta
AU  - Gamarro, Francisco
AU  - Šolaja, Bogdan A.
PY  - 2019
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/3288
PB  - Elsevier
T2  - European Journal of Medicinal Chemistry
T1  - Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010
UR  - https://hdl.handle.net/21.15107/rcub_cherry_3288
ER  - 

@misc{
author = "Manzano, Jose Ignacio and Konstantinović, Jelena M. and Scaccabarozzi, Diletta and Perea, Ana and Pavić, Aleksandar and Cavicchini, Loredana and Basilico, Nicoletta and Gamarro, Francisco and Šolaja, Bogdan A.",
year = "2019",
publisher = "Elsevier",
journal = "European Journal of Medicinal Chemistry",
title = "Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010",
url = "https://hdl.handle.net/21.15107/rcub_cherry_3288"
}

Manzano, J. I., Konstantinović, J. M., Scaccabarozzi, D., Perea, A., Pavić, A., Cavicchini, L., Basilico, N., Gamarro, F.,& Šolaja, B. A.. (2019). Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010. in European Journal of Medicinal Chemistry
Elsevier..
https://hdl.handle.net/21.15107/rcub_cherry_3288

Manzano JI, Konstantinović JM, Scaccabarozzi D, Perea A, Pavić A, Cavicchini L, Basilico N, Gamarro F, Šolaja BA. Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010. in European Journal of Medicinal Chemistry. 2019;.
https://hdl.handle.net/21.15107/rcub_cherry_3288 .

Manzano, Jose Ignacio, Konstantinović, Jelena M., Scaccabarozzi, Diletta, Perea, Ana, Pavić, Aleksandar, Cavicchini, Loredana, Basilico, Nicoletta, Gamarro, Francisco, Šolaja, Bogdan A., "Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010" in European Journal of Medicinal Chemistry (2019),
https://hdl.handle.net/21.15107/rcub_cherry_3288 .

TY  - JOUR
AU  - Selaković, Života
AU  - Tran, J.P.
AU  - Kota, K.P.
AU  - Lazić, Marija
AU  - Retterer, C.
AU  - Besh, R.
AU  - Panchal, R.G.
AU  - Soloveva, V.
AU  - Sean, V.A.
AU  - Jay, W.B.
AU  - Pavić, A.
AU  - Verbić, Tatjana
AU  - Vasiljević, Branka
AU  - Kuehl, K.
AU  - Duplantier, A.J.
AU  - Bavari, S.
AU  - Mudhasani, R.
AU  - Šolaja, Bogdan A.
PY  - 2019
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2966
AB  - Ebola virus (EBOV) causes a deadly hemorrhagic fever in humans and non-human primates. There is currently no FDA-approved vaccine or medication to counter this disease. Here, we report on the design, synthesis and anti-viral activities of two classes of compounds which show high potency against EBOV in both in vitro cell culture assays and in vivo mouse models Ebola viral disease. These compounds incorporate the structural features of cationic amphiphilic drugs (CAD), i.e they possess both a hydrophobic domain and a hydrophilic domain consisting of an ionizable amine functional group. These structural features enable easily diffusion into cells but once inside an acidic compartment their amine groups became protonated, ionized and remain trapped inside the acidic compartments such as late endosomes and lysosomes. These compounds, by virtue of their lysomotrophic functions, blocked EBOV entry. However, unlike other drugs containing a CAD moiety including chloroquine and amodiaquine, compounds reported in this study display faster kinetics of accumulation in the lysosomes, robust expansion of late endosome/lysosomes, relatively more potent suppression of lysosome fusion with other vesicular compartments and inhibition of cathepsins activities, all of which play a vital role in anti-EBOV activity. Furthermore, the diazachrysene 2 (ZSML08) that showed most potent activity against EBOV in in vitro cell culture assays also showed significant survival benefit with 100% protection in mouse models of Ebola virus disease, at a low dose of 10 mg/kg/day. Lastly, toxicity studies in vivo using zebrafish models suggest no developmental defects or toxicity associated with these compounds. Overall, these studies describe two new pharmacophores that by virtue of being potent lysosomotrophs, display potent anti-EBOV activities both in vitro and in vivo animal models of EBOV disease. © 2018 Elsevier Masson SAS
PB  - Elsevier
T2  - European Journal of Medicinal Chemistry
T1  - Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action
VL  - 162
SP  - 32
EP  - 50
DO  - 10.1016/j.ejmech.2018.10.061
ER  - 

@article{
author = "Selaković, Života and Tran, J.P. and Kota, K.P. and Lazić, Marija and Retterer, C. and Besh, R. and Panchal, R.G. and Soloveva, V. and Sean, V.A. and Jay, W.B. and Pavić, A. and Verbić, Tatjana and Vasiljević, Branka and Kuehl, K. and Duplantier, A.J. and Bavari, S. and Mudhasani, R. and Šolaja, Bogdan A.",
year = "2019",
abstract = "Ebola virus (EBOV) causes a deadly hemorrhagic fever in humans and non-human primates. There is currently no FDA-approved vaccine or medication to counter this disease. Here, we report on the design, synthesis and anti-viral activities of two classes of compounds which show high potency against EBOV in both in vitro cell culture assays and in vivo mouse models Ebola viral disease. These compounds incorporate the structural features of cationic amphiphilic drugs (CAD), i.e they possess both a hydrophobic domain and a hydrophilic domain consisting of an ionizable amine functional group. These structural features enable easily diffusion into cells but once inside an acidic compartment their amine groups became protonated, ionized and remain trapped inside the acidic compartments such as late endosomes and lysosomes. These compounds, by virtue of their lysomotrophic functions, blocked EBOV entry. However, unlike other drugs containing a CAD moiety including chloroquine and amodiaquine, compounds reported in this study display faster kinetics of accumulation in the lysosomes, robust expansion of late endosome/lysosomes, relatively more potent suppression of lysosome fusion with other vesicular compartments and inhibition of cathepsins activities, all of which play a vital role in anti-EBOV activity. Furthermore, the diazachrysene 2 (ZSML08) that showed most potent activity against EBOV in in vitro cell culture assays also showed significant survival benefit with 100% protection in mouse models of Ebola virus disease, at a low dose of 10 mg/kg/day. Lastly, toxicity studies in vivo using zebrafish models suggest no developmental defects or toxicity associated with these compounds. Overall, these studies describe two new pharmacophores that by virtue of being potent lysosomotrophs, display potent anti-EBOV activities both in vitro and in vivo animal models of EBOV disease. © 2018 Elsevier Masson SAS",
publisher = "Elsevier",
journal = "European Journal of Medicinal Chemistry",
title = "Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action",
volume = "162",
pages = "32-50",
doi = "10.1016/j.ejmech.2018.10.061"
}

Selaković, Ž., Tran, J.P., Kota, K.P., Lazić, M., Retterer, C., Besh, R., Panchal, R.G., Soloveva, V., Sean, V.A., Jay, W.B., Pavić, A., Verbić, T., Vasiljević, B., Kuehl, K., Duplantier, A.J., Bavari, S., Mudhasani, R.,& Šolaja, B. A.. (2019). Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. in European Journal of Medicinal Chemistry
Elsevier., 162, 32-50.
https://doi.org/10.1016/j.ejmech.2018.10.061

Selaković Ž, Tran J, Kota K, Lazić M, Retterer C, Besh R, Panchal R, Soloveva V, Sean V, Jay W, Pavić A, Verbić T, Vasiljević B, Kuehl K, Duplantier A, Bavari S, Mudhasani R, Šolaja BA. Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. in European Journal of Medicinal Chemistry. 2019;162:32-50.
doi:10.1016/j.ejmech.2018.10.061 .

Selaković, Života, Tran, J.P., Kota, K.P., Lazić, Marija, Retterer, C., Besh, R., Panchal, R.G., Soloveva, V., Sean, V.A., Jay, W.B., Pavić, A., Verbić, Tatjana, Vasiljević, Branka, Kuehl, K., Duplantier, A.J., Bavari, S., Mudhasani, R., Šolaja, Bogdan A., "Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action" in European Journal of Medicinal Chemistry, 162 (2019):32-50,
https://doi.org/10.1016/j.ejmech.2018.10.061 . .

TY  - DATA
AU  - Selaković, Života
AU  - Tran, J.P.
AU  - Kota, K.P.
AU  - Lazić, Marija
AU  - Retterer, C.
AU  - Besh, R.
AU  - Panchal, R.G.
AU  - Soloveva, V.
AU  - Sean, V.A.
AU  - Jay, W.B.
AU  - Pavić, A.
AU  - Verbić, Tatjana
AU  - Vasiljević, Branka
AU  - Kuehl, K.
AU  - Duplantier, A.J.
AU  - Bavari, S.
AU  - Mudhasani, R.
AU  - Šolaja, Bogdan A.
PY  - 2019
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2967
T2  - European Journal of Medicinal Chemistry
T1  - Supplementary data for article: Selaković, Ž.; Tran, J. P.; Kota, K. P.; Lazić, M.; Retterer, C.; Besh, R.; Panchal, R. G.; Soloveva, V.; Sean, V. A.; Jay, W. B.; et al. Second Generation of Diazachrysenes: Protection of Ebola Virus Infected Mice and Mechanism of Action. European Journal of Medicinal Chemistry 2019, 162, 32–50. https://doi.org/10.1016/j.ejmech.2018.10.061
UR  - https://hdl.handle.net/21.15107/rcub_cherry_2967
ER  - 

@misc{
author = "Selaković, Života and Tran, J.P. and Kota, K.P. and Lazić, Marija and Retterer, C. and Besh, R. and Panchal, R.G. and Soloveva, V. and Sean, V.A. and Jay, W.B. and Pavić, A. and Verbić, Tatjana and Vasiljević, Branka and Kuehl, K. and Duplantier, A.J. and Bavari, S. and Mudhasani, R. and Šolaja, Bogdan A.",
year = "2019",
journal = "European Journal of Medicinal Chemistry",
title = "Supplementary data for article: Selaković, Ž.; Tran, J. P.; Kota, K. P.; Lazić, M.; Retterer, C.; Besh, R.; Panchal, R. G.; Soloveva, V.; Sean, V. A.; Jay, W. B.; et al. Second Generation of Diazachrysenes: Protection of Ebola Virus Infected Mice and Mechanism of Action. European Journal of Medicinal Chemistry 2019, 162, 32–50. https://doi.org/10.1016/j.ejmech.2018.10.061",
url = "https://hdl.handle.net/21.15107/rcub_cherry_2967"
}

Selaković, Ž., Tran, J.P., Kota, K.P., Lazić, M., Retterer, C., Besh, R., Panchal, R.G., Soloveva, V., Sean, V.A., Jay, W.B., Pavić, A., Verbić, T., Vasiljević, B., Kuehl, K., Duplantier, A.J., Bavari, S., Mudhasani, R.,& Šolaja, B. A.. (2019). Supplementary data for article: Selaković, Ž.; Tran, J. P.; Kota, K. P.; Lazić, M.; Retterer, C.; Besh, R.; Panchal, R. G.; Soloveva, V.; Sean, V. A.; Jay, W. B.; et al. Second Generation of Diazachrysenes: Protection of Ebola Virus Infected Mice and Mechanism of Action. European Journal of Medicinal Chemistry 2019, 162, 32–50. https://doi.org/10.1016/j.ejmech.2018.10.061. in European Journal of Medicinal Chemistry.
https://hdl.handle.net/21.15107/rcub_cherry_2967

Selaković Ž, Tran J, Kota K, Lazić M, Retterer C, Besh R, Panchal R, Soloveva V, Sean V, Jay W, Pavić A, Verbić T, Vasiljević B, Kuehl K, Duplantier A, Bavari S, Mudhasani R, Šolaja BA. Supplementary data for article: Selaković, Ž.; Tran, J. P.; Kota, K. P.; Lazić, M.; Retterer, C.; Besh, R.; Panchal, R. G.; Soloveva, V.; Sean, V. A.; Jay, W. B.; et al. Second Generation of Diazachrysenes: Protection of Ebola Virus Infected Mice and Mechanism of Action. European Journal of Medicinal Chemistry 2019, 162, 32–50. https://doi.org/10.1016/j.ejmech.2018.10.061. in European Journal of Medicinal Chemistry. 2019;.
https://hdl.handle.net/21.15107/rcub_cherry_2967 .

Selaković, Života, Tran, J.P., Kota, K.P., Lazić, Marija, Retterer, C., Besh, R., Panchal, R.G., Soloveva, V., Sean, V.A., Jay, W.B., Pavić, A., Verbić, Tatjana, Vasiljević, Branka, Kuehl, K., Duplantier, A.J., Bavari, S., Mudhasani, R., Šolaja, Bogdan A., "Supplementary data for article: Selaković, Ž.; Tran, J. P.; Kota, K. P.; Lazić, M.; Retterer, C.; Besh, R.; Panchal, R. G.; Soloveva, V.; Sean, V. A.; Jay, W. B.; et al. Second Generation of Diazachrysenes: Protection of Ebola Virus Infected Mice and Mechanism of Action. European Journal of Medicinal Chemistry 2019, 162, 32–50. https://doi.org/10.1016/j.ejmech.2018.10.061" in European Journal of Medicinal Chemistry (2019),
https://hdl.handle.net/21.15107/rcub_cherry_2967 .

TY  - JOUR
AU  - Selaković, Života
AU  - Tran, J.P.
AU  - Kota, K.P.
AU  - Lazić, Marija
AU  - Retterer, C.
AU  - Besh, R.
AU  - Panchal, R.G.
AU  - Soloveva, V.
AU  - Sean, V.A.
AU  - Jay, W.B.
AU  - Pavić, A.
AU  - Verbić, Tatjana
AU  - Vasiljević, Branka
AU  - Kuehl, K.
AU  - Duplantier, A.J.
AU  - Bavari, S.
AU  - Mudhasani, R.
AU  - Šolaja, Bogdan A.
PY  - 2019
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/360
AB  - Ebola virus (EBOV) causes a deadly hemorrhagic fever in humans and non-human primates. There is currently no FDA-approved vaccine or medication to counter this disease. Here, we report on the design, synthesis and anti-viral activities of two classes of compounds which show high potency against EBOV in both in vitro cell culture assays and in vivo mouse models Ebola viral disease. These compounds incorporate the structural features of cationic amphiphilic drugs (CAD), i.e they possess both a hydrophobic domain and a hydrophilic domain consisting of an ionizable amine functional group. These structural features enable easily diffusion into cells but once inside an acidic compartment their amine groups became protonated, ionized and remain trapped inside the acidic compartments such as late endosomes and lysosomes. These compounds, by virtue of their lysomotrophic functions, blocked EBOV entry. However, unlike other drugs containing a CAD moiety including chloroquine and amodiaquine, compounds reported in this study display faster kinetics of accumulation in the lysosomes, robust expansion of late endosome/lysosomes, relatively more potent suppression of lysosome fusion with other vesicular compartments and inhibition of cathepsins activities, all of which play a vital role in anti-EBOV activity. Furthermore, the diazachrysene 2 (ZSML08) that showed most potent activity against EBOV in in vitro cell culture assays also showed significant survival benefit with 100% protection in mouse models of Ebola virus disease, at a low dose of 10 mg/kg/day. Lastly, toxicity studies in vivo using zebrafish models suggest no developmental defects or toxicity associated with these compounds. Overall, these studies describe two new pharmacophores that by virtue of being potent lysosomotrophs, display potent anti-EBOV activities both in vitro and in vivo animal models of EBOV disease. © 2018 Elsevier Masson SAS
T2  - European Journal of Medicinal Chemistry
T1  - Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action
VL  - 162
SP  - 32
EP  - 50
DO  - 10.1016/j.ejmech.2018.10.061
ER  - 

@article{
author = "Selaković, Života and Tran, J.P. and Kota, K.P. and Lazić, Marija and Retterer, C. and Besh, R. and Panchal, R.G. and Soloveva, V. and Sean, V.A. and Jay, W.B. and Pavić, A. and Verbić, Tatjana and Vasiljević, Branka and Kuehl, K. and Duplantier, A.J. and Bavari, S. and Mudhasani, R. and Šolaja, Bogdan A.",
year = "2019",
abstract = "Ebola virus (EBOV) causes a deadly hemorrhagic fever in humans and non-human primates. There is currently no FDA-approved vaccine or medication to counter this disease. Here, we report on the design, synthesis and anti-viral activities of two classes of compounds which show high potency against EBOV in both in vitro cell culture assays and in vivo mouse models Ebola viral disease. These compounds incorporate the structural features of cationic amphiphilic drugs (CAD), i.e they possess both a hydrophobic domain and a hydrophilic domain consisting of an ionizable amine functional group. These structural features enable easily diffusion into cells but once inside an acidic compartment their amine groups became protonated, ionized and remain trapped inside the acidic compartments such as late endosomes and lysosomes. These compounds, by virtue of their lysomotrophic functions, blocked EBOV entry. However, unlike other drugs containing a CAD moiety including chloroquine and amodiaquine, compounds reported in this study display faster kinetics of accumulation in the lysosomes, robust expansion of late endosome/lysosomes, relatively more potent suppression of lysosome fusion with other vesicular compartments and inhibition of cathepsins activities, all of which play a vital role in anti-EBOV activity. Furthermore, the diazachrysene 2 (ZSML08) that showed most potent activity against EBOV in in vitro cell culture assays also showed significant survival benefit with 100% protection in mouse models of Ebola virus disease, at a low dose of 10 mg/kg/day. Lastly, toxicity studies in vivo using zebrafish models suggest no developmental defects or toxicity associated with these compounds. Overall, these studies describe two new pharmacophores that by virtue of being potent lysosomotrophs, display potent anti-EBOV activities both in vitro and in vivo animal models of EBOV disease. © 2018 Elsevier Masson SAS",
journal = "European Journal of Medicinal Chemistry",
title = "Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action",
volume = "162",
pages = "32-50",
doi = "10.1016/j.ejmech.2018.10.061"
}

Selaković, Ž., Tran, J.P., Kota, K.P., Lazić, M., Retterer, C., Besh, R., Panchal, R.G., Soloveva, V., Sean, V.A., Jay, W.B., Pavić, A., Verbić, T., Vasiljević, B., Kuehl, K., Duplantier, A.J., Bavari, S., Mudhasani, R.,& Šolaja, B. A.. (2019). Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. in European Journal of Medicinal Chemistry, 162, 32-50.
https://doi.org/10.1016/j.ejmech.2018.10.061

Selaković Ž, Tran J, Kota K, Lazić M, Retterer C, Besh R, Panchal R, Soloveva V, Sean V, Jay W, Pavić A, Verbić T, Vasiljević B, Kuehl K, Duplantier A, Bavari S, Mudhasani R, Šolaja BA. Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. in European Journal of Medicinal Chemistry. 2019;162:32-50.
doi:10.1016/j.ejmech.2018.10.061 .

Selaković, Života, Tran, J.P., Kota, K.P., Lazić, Marija, Retterer, C., Besh, R., Panchal, R.G., Soloveva, V., Sean, V.A., Jay, W.B., Pavić, A., Verbić, Tatjana, Vasiljević, Branka, Kuehl, K., Duplantier, A.J., Bavari, S., Mudhasani, R., Šolaja, Bogdan A., "Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action" in European Journal of Medicinal Chemistry, 162 (2019):32-50,
https://doi.org/10.1016/j.ejmech.2018.10.061 . .

TY  - DATA
AU  - Konstantinović, Jelena M.
AU  - Kiris, Erkan
AU  - Kota, Krishna P.
AU  - Kugelman-Tonos, Johanny
AU  - Videnović, Milica
AU  - Cazares, Lisa H.
AU  - Terzić-Jovanović, Nataša
AU  - Verbić, Tatjana
AU  - Anđelković, Boban D.
AU  - Duplantier, Allen J.
AU  - Bavari, Sina
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/3039
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710
UR  - https://hdl.handle.net/21.15107/rcub_cherry_3039
ER  - 

@misc{
author = "Konstantinović, Jelena M. and Kiris, Erkan and Kota, Krishna P. and Kugelman-Tonos, Johanny and Videnović, Milica and Cazares, Lisa H. and Terzić-Jovanović, Nataša and Verbić, Tatjana and Anđelković, Boban D. and Duplantier, Allen J. and Bavari, Sina and Šolaja, Bogdan A.",
year = "2018",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710",
url = "https://hdl.handle.net/21.15107/rcub_cherry_3039"
}

Konstantinović, J. M., Kiris, E., Kota, K. P., Kugelman-Tonos, J., Videnović, M., Cazares, L. H., Terzić-Jovanović, N., Verbić, T., Anđelković, B. D., Duplantier, A. J., Bavari, S.,& Šolaja, B. A.. (2018). Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710. in Journal of Medicinal Chemistry
Amer Chemical Soc, Washington..
https://hdl.handle.net/21.15107/rcub_cherry_3039

Konstantinović JM, Kiris E, Kota KP, Kugelman-Tonos J, Videnović M, Cazares LH, Terzić-Jovanović N, Verbić T, Anđelković BD, Duplantier AJ, Bavari S, Šolaja BA. Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710. in Journal of Medicinal Chemistry. 2018;.
https://hdl.handle.net/21.15107/rcub_cherry_3039 .

Konstantinović, Jelena M., Kiris, Erkan, Kota, Krishna P., Kugelman-Tonos, Johanny, Videnović, Milica, Cazares, Lisa H., Terzić-Jovanović, Nataša, Verbić, Tatjana, Anđelković, Boban D., Duplantier, Allen J., Bavari, Sina, Šolaja, Bogdan A., "Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710" in Journal of Medicinal Chemistry (2018),
https://hdl.handle.net/21.15107/rcub_cherry_3039 .

TY  - JOUR
AU  - Marković, Olivera S.
AU  - Cvijetić, Ilija
AU  - Zlatović, Mario
AU  - Opsenica, Igor
AU  - Konstantinović, Jelena M.
AU  - Terzić-Jovanović, Nataša
AU  - Šolaja, Bogdan A.
AU  - Verbić, Tatjana
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2085
AB  - Interactions between eight in-house synthesized aminoquinolines, along with well-known chloroquine, and human serum albumin (HSA) have been studied by fluorescence spectroscopy. The synthesized aminoquinolines, despite being structurally diverse, were found to be very potent antimalarials. Fluorescence measurements indicate that three compounds having additional thiophene or benzothiophene substructure bind more strongly to HSA than other studied compounds. Competitive binding experiments indicate that these three compounds bind significantly stronger to warfarin compared to diazepam binding site. Fluorescence quenching at three temperatures (20, 25, and 37 degrees C) was analyzed using classical Stern-Volmer equation, and a static quenching mechanism was proposed. The enthalpy and entropy changes upon sulphur-containing compound-HSA interactions were calculated using Van't Hoff equation. Positive values of enthalpy and entropy changes indicate that non-specific, hydrophobic interactions are the main contributors to HSA-compound interaction. Molecular docking and calculated lipophilicity descriptors indicate the same, pointing out that the increased lipophilicity of sulphur-containing compounds might be a reason for their better binding to HSA. Obtained results might contribute to design of novel derivatives with improved-pharmacokinetic properties and drug efficacy. (C) 2017 Elsevier B.V. All rights reserved.
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
T1  - Human serum albumin binding of certain antimalarials
VL  - 192
SP  - 128
EP  - 139
DO  - 10.1016/j.saa.2017.10.061
ER  - 

@article{
author = "Marković, Olivera S. and Cvijetić, Ilija and Zlatović, Mario and Opsenica, Igor and Konstantinović, Jelena M. and Terzić-Jovanović, Nataša and Šolaja, Bogdan A. and Verbić, Tatjana",
year = "2018",
abstract = "Interactions between eight in-house synthesized aminoquinolines, along with well-known chloroquine, and human serum albumin (HSA) have been studied by fluorescence spectroscopy. The synthesized aminoquinolines, despite being structurally diverse, were found to be very potent antimalarials. Fluorescence measurements indicate that three compounds having additional thiophene or benzothiophene substructure bind more strongly to HSA than other studied compounds. Competitive binding experiments indicate that these three compounds bind significantly stronger to warfarin compared to diazepam binding site. Fluorescence quenching at three temperatures (20, 25, and 37 degrees C) was analyzed using classical Stern-Volmer equation, and a static quenching mechanism was proposed. The enthalpy and entropy changes upon sulphur-containing compound-HSA interactions were calculated using Van't Hoff equation. Positive values of enthalpy and entropy changes indicate that non-specific, hydrophobic interactions are the main contributors to HSA-compound interaction. Molecular docking and calculated lipophilicity descriptors indicate the same, pointing out that the increased lipophilicity of sulphur-containing compounds might be a reason for their better binding to HSA. Obtained results might contribute to design of novel derivatives with improved-pharmacokinetic properties and drug efficacy. (C) 2017 Elsevier B.V. All rights reserved.",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy",
title = "Human serum albumin binding of certain antimalarials",
volume = "192",
pages = "128-139",
doi = "10.1016/j.saa.2017.10.061"
}

Marković, O. S., Cvijetić, I., Zlatović, M., Opsenica, I., Konstantinović, J. M., Terzić-Jovanović, N., Šolaja, B. A.,& Verbić, T.. (2018). Human serum albumin binding of certain antimalarials. in Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
Pergamon-Elsevier Science Ltd, Oxford., 192, 128-139.
https://doi.org/10.1016/j.saa.2017.10.061

Marković OS, Cvijetić I, Zlatović M, Opsenica I, Konstantinović JM, Terzić-Jovanović N, Šolaja BA, Verbić T. Human serum albumin binding of certain antimalarials. in Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy. 2018;192:128-139.
doi:10.1016/j.saa.2017.10.061 .

Marković, Olivera S., Cvijetić, Ilija, Zlatović, Mario, Opsenica, Igor, Konstantinović, Jelena M., Terzić-Jovanović, Nataša, Šolaja, Bogdan A., Verbić, Tatjana, "Human serum albumin binding of certain antimalarials" in Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy, 192 (2018):128-139,
https://doi.org/10.1016/j.saa.2017.10.061 . .

TY  - DATA
AU  - Marković, Olivera S.
AU  - Cvijetić, Ilija
AU  - Zlatović, Mario
AU  - Opsenica, Igor
AU  - Konstantinović, Jelena M.
AU  - Terzić-Jovanović, Nataša
AU  - Šolaja, Bogdan A.
AU  - Verbić, Tatjana
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2913
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
T1  - Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061
UR  - https://hdl.handle.net/21.15107/rcub_cherry_2913
ER  - 

@misc{
author = "Marković, Olivera S. and Cvijetić, Ilija and Zlatović, Mario and Opsenica, Igor and Konstantinović, Jelena M. and Terzić-Jovanović, Nataša and Šolaja, Bogdan A. and Verbić, Tatjana",
year = "2018",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy",
title = "Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061",
url = "https://hdl.handle.net/21.15107/rcub_cherry_2913"
}

Marković, O. S., Cvijetić, I., Zlatović, M., Opsenica, I., Konstantinović, J. M., Terzić-Jovanović, N., Šolaja, B. A.,& Verbić, T.. (2018). Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061. in Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
Pergamon-Elsevier Science Ltd, Oxford..
https://hdl.handle.net/21.15107/rcub_cherry_2913

Marković OS, Cvijetić I, Zlatović M, Opsenica I, Konstantinović JM, Terzić-Jovanović N, Šolaja BA, Verbić T. Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061. in Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy. 2018;.
https://hdl.handle.net/21.15107/rcub_cherry_2913 .

Marković, Olivera S., Cvijetić, Ilija, Zlatović, Mario, Opsenica, Igor, Konstantinović, Jelena M., Terzić-Jovanović, Nataša, Šolaja, Bogdan A., Verbić, Tatjana, "Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061" in Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy (2018),
https://hdl.handle.net/21.15107/rcub_cherry_2913 .

TY  - JOUR
AU  - Videnović, Milica
AU  - Mojsin, Marija
AU  - Stevanović, Milena
AU  - Opsenica, Igor
AU  - Srdić-Rajić, Tatjana
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2233
AB  - A series of new benzothiazole-based carbamates and amides were synthesized and their antiproliferative activity was determined. Derivatives with profound activity were identified and further investigated for their possible mechanism of action. It was found that these compounds induce specific apoptosis, G2/M cell cycle arrest and decrease ROS level in MCF-7 human breast cancer cell line. Moreover, sub-micromolar antiproliferative activity of examined carbamates against NT2/D1 testicular embryonal carcinoma was shown. The most potent derivatives strongly inhibited NT2/D1 cell migration and invasiveness. (C) 2018 Elsevier Masson SAS. All rights reserved.
PB  - Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux
T2  - European Journal of Medicinal Chemistry
T1  - Benzothiazole carbamates and amides as antiproliferative species
VL  - 157
SP  - 1096
EP  - 1114
DO  - 10.1016/j.ejmech.2018.08.067
ER  - 

@article{
author = "Videnović, Milica and Mojsin, Marija and Stevanović, Milena and Opsenica, Igor and Srdić-Rajić, Tatjana and Šolaja, Bogdan A.",
year = "2018",
abstract = "A series of new benzothiazole-based carbamates and amides were synthesized and their antiproliferative activity was determined. Derivatives with profound activity were identified and further investigated for their possible mechanism of action. It was found that these compounds induce specific apoptosis, G2/M cell cycle arrest and decrease ROS level in MCF-7 human breast cancer cell line. Moreover, sub-micromolar antiproliferative activity of examined carbamates against NT2/D1 testicular embryonal carcinoma was shown. The most potent derivatives strongly inhibited NT2/D1 cell migration and invasiveness. (C) 2018 Elsevier Masson SAS. All rights reserved.",
publisher = "Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux",
journal = "European Journal of Medicinal Chemistry",
title = "Benzothiazole carbamates and amides as antiproliferative species",
volume = "157",
pages = "1096-1114",
doi = "10.1016/j.ejmech.2018.08.067"
}

Videnović, M., Mojsin, M., Stevanović, M., Opsenica, I., Srdić-Rajić, T.,& Šolaja, B. A.. (2018). Benzothiazole carbamates and amides as antiproliferative species. in European Journal of Medicinal Chemistry
Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux., 157, 1096-1114.
https://doi.org/10.1016/j.ejmech.2018.08.067

Videnović M, Mojsin M, Stevanović M, Opsenica I, Srdić-Rajić T, Šolaja BA. Benzothiazole carbamates and amides as antiproliferative species. in European Journal of Medicinal Chemistry. 2018;157:1096-1114.
doi:10.1016/j.ejmech.2018.08.067 .

Videnović, Milica, Mojsin, Marija, Stevanović, Milena, Opsenica, Igor, Srdić-Rajić, Tatjana, Šolaja, Bogdan A., "Benzothiazole carbamates and amides as antiproliferative species" in European Journal of Medicinal Chemistry, 157 (2018):1096-1114,
https://doi.org/10.1016/j.ejmech.2018.08.067 . .

TY  - JOUR
AU  - Videnović, Milica
AU  - Mojsin, Marija
AU  - Stevanović, Milena
AU  - Opsenica, Igor
AU  - Srdić-Rajić, Tatjana
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2960
AB  - A series of new benzothiazole-based carbamates and amides were synthesized and their antiproliferative activity was determined. Derivatives with profound activity were identified and further investigated for their possible mechanism of action. It was found that these compounds induce specific apoptosis, G2/M cell cycle arrest and decrease ROS level in MCF-7 human breast cancer cell line. Moreover, sub-micromolar antiproliferative activity of examined carbamates against NT2/D1 testicular embryonal carcinoma was shown. The most potent derivatives strongly inhibited NT2/D1 cell migration and invasiveness. (C) 2018 Elsevier Masson SAS. All rights reserved.
PB  - Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux
T2  - European Journal of Medicinal Chemistry
T1  - Benzothiazole carbamates and amides as antiproliferative species
VL  - 157
SP  - 1096
EP  - 1114
DO  - 10.1016/j.ejmech.2018.08.067
ER  - 

@article{
author = "Videnović, Milica and Mojsin, Marija and Stevanović, Milena and Opsenica, Igor and Srdić-Rajić, Tatjana and Šolaja, Bogdan A.",
year = "2018",
abstract = "A series of new benzothiazole-based carbamates and amides were synthesized and their antiproliferative activity was determined. Derivatives with profound activity were identified and further investigated for their possible mechanism of action. It was found that these compounds induce specific apoptosis, G2/M cell cycle arrest and decrease ROS level in MCF-7 human breast cancer cell line. Moreover, sub-micromolar antiproliferative activity of examined carbamates against NT2/D1 testicular embryonal carcinoma was shown. The most potent derivatives strongly inhibited NT2/D1 cell migration and invasiveness. (C) 2018 Elsevier Masson SAS. All rights reserved.",
publisher = "Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux",
journal = "European Journal of Medicinal Chemistry",
title = "Benzothiazole carbamates and amides as antiproliferative species",
volume = "157",
pages = "1096-1114",
doi = "10.1016/j.ejmech.2018.08.067"
}

Videnović, M., Mojsin, M., Stevanović, M., Opsenica, I., Srdić-Rajić, T.,& Šolaja, B. A.. (2018). Benzothiazole carbamates and amides as antiproliferative species. in European Journal of Medicinal Chemistry
Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux., 157, 1096-1114.
https://doi.org/10.1016/j.ejmech.2018.08.067

Videnović M, Mojsin M, Stevanović M, Opsenica I, Srdić-Rajić T, Šolaja BA. Benzothiazole carbamates and amides as antiproliferative species. in European Journal of Medicinal Chemistry. 2018;157:1096-1114.
doi:10.1016/j.ejmech.2018.08.067 .

Videnović, Milica, Mojsin, Marija, Stevanović, Milena, Opsenica, Igor, Srdić-Rajić, Tatjana, Šolaja, Bogdan A., "Benzothiazole carbamates and amides as antiproliferative species" in European Journal of Medicinal Chemistry, 157 (2018):1096-1114,
https://doi.org/10.1016/j.ejmech.2018.08.067 . .

TY  - DATA
AU  - Videnović, Milica
AU  - Mojsin, Marija
AU  - Stevanović, Milena
AU  - Opsenica, Igor
AU  - Srdić-Rajić, Tatjana
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2961
PB  - Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux
T2  - European Journal of Medicinal Chemistry
T1  - Supplementary material for the article: Videnović, M.; Mojsin, M.; Stevanović, M.; Opsenica, I.; Srdić-Rajić, T.; Šolaja, B. Benzothiazole Carbamates and Amides as Antiproliferative Species. Eur. J. Med. Chem. 2018, 157, 1096–1114. https://doi.org/10.1016/j.ejmech.2018.08.067
VL  - 157
SP  - 1096
EP  - 1114
UR  - https://hdl.handle.net/21.15107/rcub_cherry_2961
ER  - 

@misc{
author = "Videnović, Milica and Mojsin, Marija and Stevanović, Milena and Opsenica, Igor and Srdić-Rajić, Tatjana and Šolaja, Bogdan A.",
year = "2018",
publisher = "Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux",
journal = "European Journal of Medicinal Chemistry",
title = "Supplementary material for the article: Videnović, M.; Mojsin, M.; Stevanović, M.; Opsenica, I.; Srdić-Rajić, T.; Šolaja, B. Benzothiazole Carbamates and Amides as Antiproliferative Species. Eur. J. Med. Chem. 2018, 157, 1096–1114. https://doi.org/10.1016/j.ejmech.2018.08.067",
volume = "157",
pages = "1096-1114",
url = "https://hdl.handle.net/21.15107/rcub_cherry_2961"
}

Videnović, M., Mojsin, M., Stevanović, M., Opsenica, I., Srdić-Rajić, T.,& Šolaja, B. A.. (2018). Supplementary material for the article: Videnović, M.; Mojsin, M.; Stevanović, M.; Opsenica, I.; Srdić-Rajić, T.; Šolaja, B. Benzothiazole Carbamates and Amides as Antiproliferative Species. Eur. J. Med. Chem. 2018, 157, 1096–1114. https://doi.org/10.1016/j.ejmech.2018.08.067. in European Journal of Medicinal Chemistry
Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux., 157, 1096-1114.
https://hdl.handle.net/21.15107/rcub_cherry_2961

Videnović M, Mojsin M, Stevanović M, Opsenica I, Srdić-Rajić T, Šolaja BA. Supplementary material for the article: Videnović, M.; Mojsin, M.; Stevanović, M.; Opsenica, I.; Srdić-Rajić, T.; Šolaja, B. Benzothiazole Carbamates and Amides as Antiproliferative Species. Eur. J. Med. Chem. 2018, 157, 1096–1114. https://doi.org/10.1016/j.ejmech.2018.08.067. in European Journal of Medicinal Chemistry. 2018;157:1096-1114.
https://hdl.handle.net/21.15107/rcub_cherry_2961 .

Videnović, Milica, Mojsin, Marija, Stevanović, Milena, Opsenica, Igor, Srdić-Rajić, Tatjana, Šolaja, Bogdan A., "Supplementary material for the article: Videnović, M.; Mojsin, M.; Stevanović, M.; Opsenica, I.; Srdić-Rajić, T.; Šolaja, B. Benzothiazole Carbamates and Amides as Antiproliferative Species. Eur. J. Med. Chem. 2018, 157, 1096–1114. https://doi.org/10.1016/j.ejmech.2018.08.067" in European Journal of Medicinal Chemistry, 157 (2018):1096-1114,
https://hdl.handle.net/21.15107/rcub_cherry_2961 .

TY  - CONF
AU  - Videnović, Milica
AU  - Mojsin, Marija
AU  - Srdić-Rajić, Tatjana
AU  - Opsenica, Igor
AU  - Stevanović, Milena
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/5348
C3  - 55. Savetovanje Srpskog hemijskog društva, Novi Sad, 8. i 9. jun 2018.
T1  - Potencijalno antimetastatsko i antiproliferativno dejstvo derivata benzotiazola na ćelije embrionalnog humanog teratokarcinoma NT2/D1
T1  - Potential antimetastatic and antiproliferative activity of benzothiazole derivatives against NT2/D1 embryonal human teratocarcinoma cell line
VL  - 87
EP  - 87
UR  - https://hdl.handle.net/21.15107/rcub_cherry_5348
ER  - 

@conference{
author = "Videnović, Milica and Mojsin, Marija and Srdić-Rajić, Tatjana and Opsenica, Igor and Stevanović, Milena and Šolaja, Bogdan A.",
year = "2018",
journal = "55. Savetovanje Srpskog hemijskog društva, Novi Sad, 8. i 9. jun 2018.",
title = "Potencijalno antimetastatsko i antiproliferativno dejstvo derivata benzotiazola na ćelije embrionalnog humanog teratokarcinoma NT2/D1, Potential antimetastatic and antiproliferative activity of benzothiazole derivatives against NT2/D1 embryonal human teratocarcinoma cell line",
volume = "87",
pages = "87",
url = "https://hdl.handle.net/21.15107/rcub_cherry_5348"
}

Videnović, M., Mojsin, M., Srdić-Rajić, T., Opsenica, I., Stevanović, M.,& Šolaja, B. A.. (2018). Potencijalno antimetastatsko i antiproliferativno dejstvo derivata benzotiazola na ćelije embrionalnog humanog teratokarcinoma NT2/D1. in 55. Savetovanje Srpskog hemijskog društva, Novi Sad, 8. i 9. jun 2018., 87.
https://hdl.handle.net/21.15107/rcub_cherry_5348

Videnović M, Mojsin M, Srdić-Rajić T, Opsenica I, Stevanović M, Šolaja BA. Potencijalno antimetastatsko i antiproliferativno dejstvo derivata benzotiazola na ćelije embrionalnog humanog teratokarcinoma NT2/D1. in 55. Savetovanje Srpskog hemijskog društva, Novi Sad, 8. i 9. jun 2018.. 2018;87:null-87.
https://hdl.handle.net/21.15107/rcub_cherry_5348 .

Videnović, Milica, Mojsin, Marija, Srdić-Rajić, Tatjana, Opsenica, Igor, Stevanović, Milena, Šolaja, Bogdan A., "Potencijalno antimetastatsko i antiproliferativno dejstvo derivata benzotiazola na ćelije embrionalnog humanog teratokarcinoma NT2/D1" in 55. Savetovanje Srpskog hemijskog društva, Novi Sad, 8. i 9. jun 2018., 87 (2018),
https://hdl.handle.net/21.15107/rcub_cherry_5348 .

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Videnović, Milica
AU  - Orsini, Stefania
AU  - Bogojević, Katarina
AU  - D'Alessandro, Sarah
AU  - Scaccabarozzi, Diletta
AU  - Terzić-Jovanović, Nataša
AU  - Gradoni, Luigi
AU  - Basilico, Nicoletta
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2948
AB  - In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.
PB  - Amer Chemical Soc, Washington
T2  - ACS Medicinal Chemistry Letters
T1  - Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
VL  - 9
IS  - 7
SP  - 629
EP  - 634
DO  - 10.1021/acsmedchemlett.8b00053
ER  - 

@article{
author = "Konstantinović, Jelena M. and Videnović, Milica and Orsini, Stefania and Bogojević, Katarina and D'Alessandro, Sarah and Scaccabarozzi, Diletta and Terzić-Jovanović, Nataša and Gradoni, Luigi and Basilico, Nicoletta and Šolaja, Bogdan A.",
year = "2018",
abstract = "In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.",
publisher = "Amer Chemical Soc, Washington",
journal = "ACS Medicinal Chemistry Letters",
title = "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice",
volume = "9",
number = "7",
pages = "629-634",
doi = "10.1021/acsmedchemlett.8b00053"
}

Konstantinović, J. M., Videnović, M., Orsini, S., Bogojević, K., D'Alessandro, S., Scaccabarozzi, D., Terzić-Jovanović, N., Gradoni, L., Basilico, N.,& Šolaja, B. A.. (2018). Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. in ACS Medicinal Chemistry Letters
Amer Chemical Soc, Washington., 9(7), 629-634.
https://doi.org/10.1021/acsmedchemlett.8b00053

Konstantinović JM, Videnović M, Orsini S, Bogojević K, D'Alessandro S, Scaccabarozzi D, Terzić-Jovanović N, Gradoni L, Basilico N, Šolaja BA. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. in ACS Medicinal Chemistry Letters. 2018;9(7):629-634.
doi:10.1021/acsmedchemlett.8b00053 .

Konstantinović, Jelena M., Videnović, Milica, Orsini, Stefania, Bogojević, Katarina, D'Alessandro, Sarah, Scaccabarozzi, Diletta, Terzić-Jovanović, Nataša, Gradoni, Luigi, Basilico, Nicoletta, Šolaja, Bogdan A., "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice" in ACS Medicinal Chemistry Letters, 9, no. 7 (2018):629-634,
https://doi.org/10.1021/acsmedchemlett.8b00053 . .

TY  - DATA
AU  - Konstantinović, Jelena M.
AU  - Videnović, Milica
AU  - Orsini, Stefania
AU  - Bogojević, Katarina
AU  - D'Alessandro, Sarah
AU  - Scaccabarozzi, Diletta
AU  - Terzić-Jovanović, Nataša
AU  - Gradoni, Luigi
AU  - Basilico, Nicoletta
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2949
PB  - Amer Chemical Soc, Washington
T2  - ACS Medicinal Chemistry Letters
T1  - Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053
UR  - https://hdl.handle.net/21.15107/rcub_cherry_2949
ER  - 

@misc{
author = "Konstantinović, Jelena M. and Videnović, Milica and Orsini, Stefania and Bogojević, Katarina and D'Alessandro, Sarah and Scaccabarozzi, Diletta and Terzić-Jovanović, Nataša and Gradoni, Luigi and Basilico, Nicoletta and Šolaja, Bogdan A.",
year = "2018",
publisher = "Amer Chemical Soc, Washington",
journal = "ACS Medicinal Chemistry Letters",
title = "Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053",
url = "https://hdl.handle.net/21.15107/rcub_cherry_2949"
}

Konstantinović, J. M., Videnović, M., Orsini, S., Bogojević, K., D'Alessandro, S., Scaccabarozzi, D., Terzić-Jovanović, N., Gradoni, L., Basilico, N.,& Šolaja, B. A.. (2018). Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053. in ACS Medicinal Chemistry Letters
Amer Chemical Soc, Washington..
https://hdl.handle.net/21.15107/rcub_cherry_2949

Konstantinović JM, Videnović M, Orsini S, Bogojević K, D'Alessandro S, Scaccabarozzi D, Terzić-Jovanović N, Gradoni L, Basilico N, Šolaja BA. Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053. in ACS Medicinal Chemistry Letters. 2018;.
https://hdl.handle.net/21.15107/rcub_cherry_2949 .

Konstantinović, Jelena M., Videnović, Milica, Orsini, Stefania, Bogojević, Katarina, D'Alessandro, Sarah, Scaccabarozzi, Diletta, Terzić-Jovanović, Nataša, Gradoni, Luigi, Basilico, Nicoletta, Šolaja, Bogdan A., "Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053" in ACS Medicinal Chemistry Letters (2018),
https://hdl.handle.net/21.15107/rcub_cherry_2949 .

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Kiris, Erkan
AU  - Kota, Krishna P.
AU  - Kugelman-Tonos, Johanny
AU  - Videnović, Milica
AU  - Cazares, Lisa H.
AU  - Terzić-Jovanović, Nataša
AU  - Verbić, Tatjana
AU  - Anđelković, Boban D.
AU  - Duplantier, Allen J.
AU  - Bavari, Sina
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2099
AB  - The synthesis and inhibitory potencies against botulinum neurotoxin serotype A light chain (BoNT/A LC) using in vitro HPLC based enzymatic assay for various steroidal, benzothiophene, thiophene, and adamantane 4-aminoquinoline derivatives are described. In addition, the compounds were evaluated for the activity against BoNT/A holotoxin in mouse embryonic stem cell derived motor neurons. Steroidal derivative 16 showed remarkable protection (up to 89% of uncleaved SNAP-25) even when administered 30 min postintoxication. This appears to be the first example of LC inhibitors antagonizing BoNT intoxication in mouse embryonic stem cell derived motor neurons (mES-MNs) in a postexposure model. Oral administration of 16 was well tolerated in the mouse up to 600 mg/kg, q.d. Although adequate unbound drug levels were not achieved at this dose, the favorable in vitro ADMET results strongly support further work in this series.
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model
VL  - 61
IS  - 4
SP  - 1595
EP  - 1608
DO  - 10.1021/acs.jmedchem.7b01710
ER  - 

@article{
author = "Konstantinović, Jelena M. and Kiris, Erkan and Kota, Krishna P. and Kugelman-Tonos, Johanny and Videnović, Milica and Cazares, Lisa H. and Terzić-Jovanović, Nataša and Verbić, Tatjana and Anđelković, Boban D. and Duplantier, Allen J. and Bavari, Sina and Šolaja, Bogdan A.",
year = "2018",
abstract = "The synthesis and inhibitory potencies against botulinum neurotoxin serotype A light chain (BoNT/A LC) using in vitro HPLC based enzymatic assay for various steroidal, benzothiophene, thiophene, and adamantane 4-aminoquinoline derivatives are described. In addition, the compounds were evaluated for the activity against BoNT/A holotoxin in mouse embryonic stem cell derived motor neurons. Steroidal derivative 16 showed remarkable protection (up to 89% of uncleaved SNAP-25) even when administered 30 min postintoxication. This appears to be the first example of LC inhibitors antagonizing BoNT intoxication in mouse embryonic stem cell derived motor neurons (mES-MNs) in a postexposure model. Oral administration of 16 was well tolerated in the mouse up to 600 mg/kg, q.d. Although adequate unbound drug levels were not achieved at this dose, the favorable in vitro ADMET results strongly support further work in this series.",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model",
volume = "61",
number = "4",
pages = "1595-1608",
doi = "10.1021/acs.jmedchem.7b01710"
}

Konstantinović, J. M., Kiris, E., Kota, K. P., Kugelman-Tonos, J., Videnović, M., Cazares, L. H., Terzić-Jovanović, N., Verbić, T., Anđelković, B. D., Duplantier, A. J., Bavari, S.,& Šolaja, B. A.. (2018). New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. in Journal of Medicinal Chemistry
Amer Chemical Soc, Washington., 61(4), 1595-1608.
https://doi.org/10.1021/acs.jmedchem.7b01710

Konstantinović JM, Kiris E, Kota KP, Kugelman-Tonos J, Videnović M, Cazares LH, Terzić-Jovanović N, Verbić T, Anđelković BD, Duplantier AJ, Bavari S, Šolaja BA. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. in Journal of Medicinal Chemistry. 2018;61(4):1595-1608.
doi:10.1021/acs.jmedchem.7b01710 .

Konstantinović, Jelena M., Kiris, Erkan, Kota, Krishna P., Kugelman-Tonos, Johanny, Videnović, Milica, Cazares, Lisa H., Terzić-Jovanović, Nataša, Verbić, Tatjana, Anđelković, Boban D., Duplantier, Allen J., Bavari, Sina, Šolaja, Bogdan A., "New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model" in Journal of Medicinal Chemistry, 61, no. 4 (2018):1595-1608,
https://doi.org/10.1021/acs.jmedchem.7b01710 . .

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Videnović, Milica
AU  - Orsini, Stefania
AU  - Bogojević, Katarina
AU  - D'Alessandro, Sarah
AU  - Scaccabarozzi, Diletta
AU  - Terzić-Jovanović, Nataša
AU  - Gradoni, Luigi
AU  - Basilico, Nicoletta
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2209
AB  - In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.
PB  - Amer Chemical Soc, Washington
T2  - ACS Medicinal Chemistry Letters
T1  - Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
VL  - 9
IS  - 7
SP  - 629
EP  - 634
DO  - 10.1021/acsmedchemlett.8b00053
ER  - 

@article{
author = "Konstantinović, Jelena M. and Videnović, Milica and Orsini, Stefania and Bogojević, Katarina and D'Alessandro, Sarah and Scaccabarozzi, Diletta and Terzić-Jovanović, Nataša and Gradoni, Luigi and Basilico, Nicoletta and Šolaja, Bogdan A.",
year = "2018",
abstract = "In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.",
publisher = "Amer Chemical Soc, Washington",
journal = "ACS Medicinal Chemistry Letters",
title = "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice",
volume = "9",
number = "7",
pages = "629-634",
doi = "10.1021/acsmedchemlett.8b00053"
}

Konstantinović, J. M., Videnović, M., Orsini, S., Bogojević, K., D'Alessandro, S., Scaccabarozzi, D., Terzić-Jovanović, N., Gradoni, L., Basilico, N.,& Šolaja, B. A.. (2018). Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. in ACS Medicinal Chemistry Letters
Amer Chemical Soc, Washington., 9(7), 629-634.
https://doi.org/10.1021/acsmedchemlett.8b00053

Konstantinović JM, Videnović M, Orsini S, Bogojević K, D'Alessandro S, Scaccabarozzi D, Terzić-Jovanović N, Gradoni L, Basilico N, Šolaja BA. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. in ACS Medicinal Chemistry Letters. 2018;9(7):629-634.
doi:10.1021/acsmedchemlett.8b00053 .

Konstantinović, Jelena M., Videnović, Milica, Orsini, Stefania, Bogojević, Katarina, D'Alessandro, Sarah, Scaccabarozzi, Diletta, Terzić-Jovanović, Nataša, Gradoni, Luigi, Basilico, Nicoletta, Šolaja, Bogdan A., "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice" in ACS Medicinal Chemistry Letters, 9, no. 7 (2018):629-634,
https://doi.org/10.1021/acsmedchemlett.8b00053 . .

TY  - CONF
AU  - Marković, Olivera S.
AU  - Konstantinović, Jelena M.
AU  - Cvijetić, Ilija 
AU  - Amézqueta, Susana
AU  - Valko, Klara
AU  - Ràfols, Clara
AU  - Polović, Natalija
AU  - Šolaja, Bogdan A.
AU  - Verbić, Tatjana
PY  - 2017
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/5959
AB  - Drug molecules in vivo may be bound to proteins and lipids in plasma and/or in tissues, or
free (unbound) in diffusion among the aqueous environment of the blood and tissues.
Data from in vitro plasma protein binding experiments that determine the fraction of
protein-bound drug are frequently used in drug discovery [1].
Human plasma proteins contain around 40 % albumin (HSA), 1-acid glycoprotein (AGP) in
much lower concentration (1-3 %) and immunoglobulins [2]. Methods used for drug –
plasma protein binding (PPB) studies are numerous and can be divided into two main
groups: separation methods (enabling the calculation of binding parameters, i.e. the number
of binding sites and their respective affinity constants) and non-separation methods
(describing predominantly qualitative parameters of the ligand-protein complex) [3].
Sometimes, results of PPB measurements obtained by different techniques are not
consistent. High binding affinity to plasma proteins is not necessarily a crucial limiting
factor for further delivery of compound to the target organ [1]. As an example, we show
the study of the interactions between HSA/AGP and an “in-house” synthesized steroidal
derivative that showed remarkable inhibitory potency against BoNT/A holotoxin in mouse
embryonic stem cell derived motor neurons [4]. A variety of experimental techniques (ITC,
HPLC, spectrofluorimetry, FTIR, and equilibrium dialysis) were used and the results were
compared highlighting the advantages and disadvatages of various techniques.
PB  - International Association of Physical Chemists
C3  - 6th IAPC Meeting Sixth World Conference on Physico-Chemical Methods in Drug Discovery  & Third World Conference on ADMET and DMPK, Zagreb, Croatia, September 4-7, 2017
T1  - Measurements of plasma protein binding – variety of experimental techniques
SP  - 30
EP  - 30
UR  - https://hdl.handle.net/21.15107/rcub_cherry_5959
ER  - 

@conference{
author = "Marković, Olivera S. and Konstantinović, Jelena M. and Cvijetić, Ilija  and Amézqueta, Susana and Valko, Klara and Ràfols, Clara and Polović, Natalija and Šolaja, Bogdan A. and Verbić, Tatjana",
year = "2017",
abstract = "Drug molecules in vivo may be bound to proteins and lipids in plasma and/or in tissues, or
free (unbound) in diffusion among the aqueous environment of the blood and tissues.
Data from in vitro plasma protein binding experiments that determine the fraction of
protein-bound drug are frequently used in drug discovery [1].
Human plasma proteins contain around 40 % albumin (HSA), 1-acid glycoprotein (AGP) in
much lower concentration (1-3 %) and immunoglobulins [2]. Methods used for drug –
plasma protein binding (PPB) studies are numerous and can be divided into two main
groups: separation methods (enabling the calculation of binding parameters, i.e. the number
of binding sites and their respective affinity constants) and non-separation methods
(describing predominantly qualitative parameters of the ligand-protein complex) [3].
Sometimes, results of PPB measurements obtained by different techniques are not
consistent. High binding affinity to plasma proteins is not necessarily a crucial limiting
factor for further delivery of compound to the target organ [1]. As an example, we show
the study of the interactions between HSA/AGP and an “in-house” synthesized steroidal
derivative that showed remarkable inhibitory potency against BoNT/A holotoxin in mouse
embryonic stem cell derived motor neurons [4]. A variety of experimental techniques (ITC,
HPLC, spectrofluorimetry, FTIR, and equilibrium dialysis) were used and the results were
compared highlighting the advantages and disadvatages of various techniques.",
publisher = "International Association of Physical Chemists",
journal = "6th IAPC Meeting Sixth World Conference on Physico-Chemical Methods in Drug Discovery  & Third World Conference on ADMET and DMPK, Zagreb, Croatia, September 4-7, 2017",
title = "Measurements of plasma protein binding – variety of experimental techniques",
pages = "30-30",
url = "https://hdl.handle.net/21.15107/rcub_cherry_5959"
}

Marković, O. S., Konstantinović, J. M., Cvijetić, I., Amézqueta, S., Valko, K., Ràfols, C., Polović, N., Šolaja, B. A.,& Verbić, T.. (2017). Measurements of plasma protein binding – variety of experimental techniques. in 6th IAPC Meeting Sixth World Conference on Physico-Chemical Methods in Drug Discovery  & Third World Conference on ADMET and DMPK, Zagreb, Croatia, September 4-7, 2017
International Association of Physical Chemists., 30-30.
https://hdl.handle.net/21.15107/rcub_cherry_5959

Marković OS, Konstantinović JM, Cvijetić I, Amézqueta S, Valko K, Ràfols C, Polović N, Šolaja BA, Verbić T. Measurements of plasma protein binding – variety of experimental techniques. in 6th IAPC Meeting Sixth World Conference on Physico-Chemical Methods in Drug Discovery  & Third World Conference on ADMET and DMPK, Zagreb, Croatia, September 4-7, 2017. 2017;:30-30.
https://hdl.handle.net/21.15107/rcub_cherry_5959 .

Marković, Olivera S., Konstantinović, Jelena M., Cvijetić, Ilija , Amézqueta, Susana, Valko, Klara, Ràfols, Clara, Polović, Natalija, Šolaja, Bogdan A., Verbić, Tatjana, "Measurements of plasma protein binding – variety of experimental techniques" in 6th IAPC Meeting Sixth World Conference on Physico-Chemical Methods in Drug Discovery  & Third World Conference on ADMET and DMPK, Zagreb, Croatia, September 4-7, 2017 (2017):30-30,
https://hdl.handle.net/21.15107/rcub_cherry_5959 .

TY  - JOUR
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Konstantinović, Jelena M.
AU  - Terzić-Jovanović, Nataša
AU  - Uzelac, Aleksandra
AU  - Bobić, Branko
AU  - Šolaja, Bogdan A.
AU  - Đurković-Đaković, Olgica
PY  - 2017
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/3214
AB  - Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of  gt = 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded  gt = 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines.
PB  - Elsevier Science Bv, Amsterdam
T2  - International Journal of Antimicrobial Agents
T1  - Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy
VL  - 50
IS  - 3
SP  - 461
EP  - 466
DO  - 10.1016/j.ijantimicag.2017.06.002
ER  - 

@article{
author = "Srbljanović, Jelena and Štajner, Tijana and Konstantinović, Jelena M. and Terzić-Jovanović, Nataša and Uzelac, Aleksandra and Bobić, Branko and Šolaja, Bogdan A. and Đurković-Đaković, Olgica",
year = "2017",
abstract = "Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of  gt = 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded  gt = 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines.",
publisher = "Elsevier Science Bv, Amsterdam",
journal = "International Journal of Antimicrobial Agents",
title = "Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy",
volume = "50",
number = "3",
pages = "461-466",
doi = "10.1016/j.ijantimicag.2017.06.002"
}

Srbljanović, J., Štajner, T., Konstantinović, J. M., Terzić-Jovanović, N., Uzelac, A., Bobić, B., Šolaja, B. A.,& Đurković-Đaković, O.. (2017). Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy. in International Journal of Antimicrobial Agents
Elsevier Science Bv, Amsterdam., 50(3), 461-466.
https://doi.org/10.1016/j.ijantimicag.2017.06.002

Srbljanović J, Štajner T, Konstantinović JM, Terzić-Jovanović N, Uzelac A, Bobić B, Šolaja BA, Đurković-Đaković O. Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy. in International Journal of Antimicrobial Agents. 2017;50(3):461-466.
doi:10.1016/j.ijantimicag.2017.06.002 .

Srbljanović, Jelena, Štajner, Tijana, Konstantinović, Jelena M., Terzić-Jovanović, Nataša, Uzelac, Aleksandra, Bobić, Branko, Šolaja, Bogdan A., Đurković-Đaković, Olgica, "Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy" in International Journal of Antimicrobial Agents, 50, no. 3 (2017):461-466,
https://doi.org/10.1016/j.ijantimicag.2017.06.002 . .