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.
TY - 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 - http://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 - 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 and Terzić-Jovanović, Nataša and Smith, P.L. and Yang, Y. and Anova, L. and Smith, K. S. and Šolaja, Bogdan",
year = "2008",
url = "http://cer.ihtm.bg.ac.rs/handle/123456789/444",
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 = "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., Terzić-Jovanović, N., Smith, P.L., Yang, Y., Anova, L., Smith, K. S.,& Šolaja, B. (2008). Mixed tetraoxanes containing the acetone subunit as antimalarials.
Bioorganic and Medicinal Chemistry
Pergamon-Elsevier Science Ltd, Oxford., 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. Bioorganic and Medicinal Chemistry. 2008;16(14):7039-7045
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" Bioorganic and Medicinal Chemistry, 16, no. 14 (2008):7039-7045,
https://doi.org/10.1016/j.bmc.2008.05.017 .
