Mixed tetraoxanes of the 4"-phenyl-substituted cyclohexyl-spirotetraoxacyclohexyl-spirocholate series have been prepared and evaluated as possible antimalarials, anti-proliferatives and antimycobacterials. The activity of the (4"R or S)-phenyl series against P falciarum D6 and W2 strains was found to be at the level of artemisinin. with two compounds. the acid 4 and the amide 6, exhibiting encouraging anti-TB activity as well. Very promising in vitro results of the said tetraoxanes were obtained against solid tumours and, in some instances. the activity against a selected number of cell lines was higher than that of the antitumor drug paclitaxel.
U ovom radu prikazana je sinteza serije mešovitih tetraoksana 4"-fenil-supstituisanih cikloheksil-spirotetraoksacikloheksil-spiroholata, a ispitana je i njihova in vitro aktivnost kao mogućih antimalarika, anti-TBC agenasa i antiproliferativnih jedinjenja. Aktivnost (4"R ili S)-fenil serije na D6 i W2 sojeve P. falciparum vrlo je slična aktivnosti poznatog antimalarika artemizinina. Izraženu anti-TBC aktivnost iskazala su jedinjenja 4 i 6, čija antiproliferativna in vitro aktivnost prema nekim kompaktnim tumorima prevazilazi aktivnost leka paklitaksela.
TY - JOUR
AU - Opsenica, Dejan M.
AU - Kyle, DE
AU - Milhous, WK
AU - Šolaja, Bogdan A.
PY - 2003
UR - https://cherry.chem.bg.ac.rs/handle/123456789/555
AB - Mixed tetraoxanes of the 4"-phenyl-substituted cyclohexyl-spirotetraoxacyclohexyl-spirocholate series have been prepared and evaluated as possible antimalarials, anti-proliferatives and antimycobacterials. The activity of the (4"R or S)-phenyl series against P falciarum D6 and W2 strains was found to be at the level of artemisinin. with two compounds. the acid 4 and the amide 6, exhibiting encouraging anti-TB activity as well. Very promising in vitro results of the said tetraoxanes were obtained against solid tumours and, in some instances. the activity against a selected number of cell lines was higher than that of the antitumor drug paclitaxel.
AB - U ovom radu prikazana je sinteza serije mešovitih tetraoksana 4"-fenil-supstituisanih cikloheksil-spirotetraoksacikloheksil-spiroholata, a ispitana je i njihova in vitro aktivnost kao mogućih antimalarika, anti-TBC agenasa i antiproliferativnih jedinjenja. Aktivnost (4"R ili S)-fenil serije na D6 i W2 sojeve P. falciparum vrlo je slična aktivnosti poznatog antimalarika artemizinina. Izraženu anti-TBC aktivnost iskazala su jedinjenja 4 i 6, čija antiproliferativna in vitro aktivnost prema nekim kompaktnim tumorima prevazilazi aktivnost leka paklitaksela.
PB - Serbian Chemical Soc, Belgrade
T2 - Journal of the Serbian Chemical Society
T1 - Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes
T1 - Antimalarijska, antimikobakterijska i antiproliferativna aktivnost fenil-supstituisanih tetraoksana
VL - 68
IS - 4-5
SP - 291
EP - 302
DO - 10.2298/JSC0305291O
ER -
@article{
author = "Opsenica, Dejan M. and Kyle, DE and Milhous, WK and Šolaja, Bogdan A.",
year = "2003",
abstract = "Mixed tetraoxanes of the 4"-phenyl-substituted cyclohexyl-spirotetraoxacyclohexyl-spirocholate series have been prepared and evaluated as possible antimalarials, anti-proliferatives and antimycobacterials. The activity of the (4"R or S)-phenyl series against P falciarum D6 and W2 strains was found to be at the level of artemisinin. with two compounds. the acid 4 and the amide 6, exhibiting encouraging anti-TB activity as well. Very promising in vitro results of the said tetraoxanes were obtained against solid tumours and, in some instances. the activity against a selected number of cell lines was higher than that of the antitumor drug paclitaxel., U ovom radu prikazana je sinteza serije mešovitih tetraoksana 4"-fenil-supstituisanih cikloheksil-spirotetraoksacikloheksil-spiroholata, a ispitana je i njihova in vitro aktivnost kao mogućih antimalarika, anti-TBC agenasa i antiproliferativnih jedinjenja. Aktivnost (4"R ili S)-fenil serije na D6 i W2 sojeve P. falciparum vrlo je slična aktivnosti poznatog antimalarika artemizinina. Izraženu anti-TBC aktivnost iskazala su jedinjenja 4 i 6, čija antiproliferativna in vitro aktivnost prema nekim kompaktnim tumorima prevazilazi aktivnost leka paklitaksela.",
publisher = "Serbian Chemical Soc, Belgrade",
journal = "Journal of the Serbian Chemical Society",
title = "Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes, Antimalarijska, antimikobakterijska i antiproliferativna aktivnost fenil-supstituisanih tetraoksana",
volume = "68",
number = "4-5",
pages = "291-302",
doi = "10.2298/JSC0305291O"
}
Opsenica, D. M., Kyle, D., Milhous, W.,& Šolaja, B. A.. (2003). Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes. in Journal of the Serbian Chemical Society
Serbian Chemical Soc, Belgrade., 68(4-5), 291-302.
https://doi.org/10.2298/JSC0305291O
Opsenica DM, Kyle D, Milhous W, Šolaja BA. Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes. in Journal of the Serbian Chemical Society. 2003;68(4-5):291-302.
doi:10.2298/JSC0305291O .
Opsenica, Dejan M., Kyle, DE, Milhous, WK, Šolaja, Bogdan A., "Antimalarial, antimycobacterial and antiproliferative activity of phenyl substituted mixed tetraoxanes" in Journal of the Serbian Chemical Society, 68, no. 4-5 (2003):291-302,
https://doi.org/10.2298/JSC0305291O . .
