Mixed tetraoxanes containing the acetone subunit as antimalarials
Само за регистроване кориснике
2008
Аутори
Opsenica, DejanTerzić-Jovanović, Nataša
Smith, P.L.
Yang, Y.
Anova, L.
Smith, K. S.
Šolaja, Bogdan
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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 ≤ 20 mg/kg/day. The diol 13 was most potent antiproliferative with GI50, TGI, LC50 MG_MID 0.98 μM, 3.80 μM, 11.22 μM, respectively. All tested compounds showed no toxic effects.
Кључне речи:
Antimalarials / Antiproliferatives / Cholic acid / Metabolic stability / Mixed steroidal tetraoxanesИзвор:
Bioorganic and Medicinal Chemistry, 2008, 16, 14, 7039-7045Издавач:
- Oxford : Pergamon-Elsevier Science Ltd
Финансирање / пројекти:
- Пероксидни антималарици и њихове химере са хинолинима: синтеза и биолошка активност (RS-MESTD-MPN2006-2010-142022)
DOI: 10.1016/j.bmc.2008.05.017
ISSN: 0968-0896
PubMed: 18550377
WoS: 000257829600042
Scopus: 2-s2.0-48949115566
Институција/група
IHTMTY - JOUR AU - Opsenica, Dejan AU - Terzić-Jovanović, Nataša AU - Smith, P.L. AU - Yang, Y. AU - Anova, L. AU - Smith, K. S. AU - Šolaja, Bogdan PY - 2008 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/444 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 ≤ 20 mg/kg/day. The diol 13 was most potent antiproliferative with GI50, TGI, LC50 MG_MID 0.98 μM, 3.80 μM, 11.22 μM, respectively. All tested compounds showed no toxic effects. PB - Oxford : Pergamon-Elsevier Science Ltd 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 and Terzić-Jovanović, Nataša and Smith, P.L. and Yang, Y. and Anova, L. and Smith, K. S. and Šolaja, Bogdan", 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 ≤ 20 mg/kg/day. The diol 13 was most potent antiproliferative with GI50, TGI, LC50 MG_MID 0.98 μM, 3.80 μM, 11.22 μM, respectively. All tested compounds showed no toxic effects.", publisher = "Oxford : Pergamon-Elsevier Science Ltd", 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., Terzić-Jovanović, N., Smith, P.L., Yang, Y., Anova, L., Smith, K. S.,& Šolaja, B.. (2008). Mixed tetraoxanes containing the acetone subunit as antimalarials. in Bioorganic and Medicinal Chemistry Oxford : Pergamon-Elsevier Science Ltd., 16(14), 7039-7045. https://doi.org/10.1016/j.bmc.2008.05.017
Opsenica D, Terzić-Jovanović N, Smith P, Yang Y, Anova L, Smith KS, Šolaja B. 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, Terzić-Jovanović, Nataša, Smith, P.L., Yang, Y., Anova, L., Smith, K. S., Šolaja, Bogdan, "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 . .