Mixed tetraoxanes containing the acetone subunit as antimalarials
Nema prikaza
Autori
Opsenica, Dejan M.Terzić-Jovanović, Nataša
Smith, Philip L.
Yang, Youngsun
Anova, Lalaine
Smith, Kirsten S.
Šolaja, Bogdan A.
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
Eleven new tetraoxanes possessing cholic acid-derived carrier and isopropylidene moiety were synthesized and were tested in vitro and in vivo. In vitro screening revealed that nine of them were more potent against CQ-resistant W2 than CQ-susceptible D6 strain and that two of them were equally or more potent than artemisinin and mefloquine against multi- drug resistant TM91C235 strain. Amine 8 cured all mice at the dose of 160 mg/kg/day, while the anilide 9 exhibited MCD lt = 20 mg/kg/day. The diol 13 was most potent antiproliferative with GI(50), TGI, LC50 MG_MID 0.98 mu M, 3.80 mu M, 11.22 mu M, respectively. All tested compounds showed no toxic effects. (c) 2008 Elsevier Ltd. All rights reserved.
Ključne reči:
mixed steroidal tetraoxanes / cholic acid / antimalarials / antiproliferatives / metabolic stabilityIzvor:
Bioorganic and Medicinal Chemistry, 2008, 16, 14, 7039-7045Izdavač:
- Pergamon-Elsevier Science Ltd, Oxford
DOI: 10.1016/j.bmc.2008.05.017
ISSN: 0968-0896
PubMed: 18550377
WoS: 000257829600042
Scopus: 2-s2.0-48949115566
Kolekcije
Institucija/grupa
Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Opsenica, Dejan M. AU - Terzić-Jovanović, Nataša AU - Smith, Philip L. AU - Yang, Youngsun AU - Anova, Lalaine AU - Smith, Kirsten S. AU - Šolaja, Bogdan A. PY - 2008 UR - https://cherry.chem.bg.ac.rs/handle/123456789/957 AB - Eleven new tetraoxanes possessing cholic acid-derived carrier and isopropylidene moiety were synthesized and were tested in vitro and in vivo. In vitro screening revealed that nine of them were more potent against CQ-resistant W2 than CQ-susceptible D6 strain and that two of them were equally or more potent than artemisinin and mefloquine against multi- drug resistant TM91C235 strain. Amine 8 cured all mice at the dose of 160 mg/kg/day, while the anilide 9 exhibited MCD lt = 20 mg/kg/day. The diol 13 was most potent antiproliferative with GI(50), TGI, LC50 MG_MID 0.98 mu M, 3.80 mu M, 11.22 mu M, respectively. All tested compounds showed no toxic effects. (c) 2008 Elsevier Ltd. All rights reserved. PB - Pergamon-Elsevier Science Ltd, Oxford T2 - Bioorganic and Medicinal Chemistry T1 - Mixed tetraoxanes containing the acetone subunit as antimalarials VL - 16 IS - 14 SP - 7039 EP - 7045 DO - 10.1016/j.bmc.2008.05.017 ER -
@article{ author = "Opsenica, Dejan M. and Terzić-Jovanović, Nataša and Smith, Philip L. and Yang, Youngsun and Anova, Lalaine and Smith, Kirsten S. and Šolaja, Bogdan A.", year = "2008", abstract = "Eleven new tetraoxanes possessing cholic acid-derived carrier and isopropylidene moiety were synthesized and were tested in vitro and in vivo. In vitro screening revealed that nine of them were more potent against CQ-resistant W2 than CQ-susceptible D6 strain and that two of them were equally or more potent than artemisinin and mefloquine against multi- drug resistant TM91C235 strain. Amine 8 cured all mice at the dose of 160 mg/kg/day, while the anilide 9 exhibited MCD lt = 20 mg/kg/day. The diol 13 was most potent antiproliferative with GI(50), TGI, LC50 MG_MID 0.98 mu M, 3.80 mu M, 11.22 mu M, respectively. All tested compounds showed no toxic effects. (c) 2008 Elsevier Ltd. All rights reserved.", publisher = "Pergamon-Elsevier Science Ltd, Oxford", journal = "Bioorganic and Medicinal Chemistry", title = "Mixed tetraoxanes containing the acetone subunit as antimalarials", volume = "16", number = "14", pages = "7039-7045", doi = "10.1016/j.bmc.2008.05.017" }
Opsenica, D. M., Terzić-Jovanović, N., Smith, P. L., Yang, Y., Anova, L., Smith, K. S.,& Šolaja, B. A.. (2008). Mixed tetraoxanes containing the acetone subunit as antimalarials. in Bioorganic and Medicinal Chemistry Pergamon-Elsevier Science Ltd, Oxford., 16(14), 7039-7045. https://doi.org/10.1016/j.bmc.2008.05.017
Opsenica DM, Terzić-Jovanović N, Smith PL, Yang Y, Anova L, Smith KS, Šolaja BA. Mixed tetraoxanes containing the acetone subunit as antimalarials. in Bioorganic and Medicinal Chemistry. 2008;16(14):7039-7045. doi:10.1016/j.bmc.2008.05.017 .
Opsenica, Dejan M., Terzić-Jovanović, Nataša, Smith, Philip L., Yang, Youngsun, Anova, Lalaine, Smith, Kirsten S., Šolaja, Bogdan A., "Mixed tetraoxanes containing the acetone subunit as antimalarials" in Bioorganic and Medicinal Chemistry, 16, no. 14 (2008):7039-7045, https://doi.org/10.1016/j.bmc.2008.05.017 . .