1. Mixed tetraoxanes containing the acetone subunit as antimalarials
- Author
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Opsenica, Dejan M., Terzić, Nataša, Smith, Philip L., Yang, Youngsun, Anova, Lalaine, Smith, Kirsten S., and Šolaja, Bogdan A.
- Subjects
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ANTIMALARIALS , *ARTEMISININ , *MEFLOQUINE , *PEROXIDES - Abstract
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 160mg/kg/day, while the anilide 9 exhibited MCD⩽20mg/kg/day. The diol 13 was most potent antiproliferative with GI50, TGI, LC50 MG_MID 0.98μM, 3.80μM, 11.22μM, respectively. All tested compounds showed no toxic effects. [Copyright &y& Elsevier]
- Published
- 2008
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