Mixed tetraoxanes containing the acetone subunit as antimalarials
AutoriOpsenica, Dejan M.
Smith, Philip L.
Smith, Kirsten S.
Šolaja, Bogdan A.
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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 stability
Izvor:Bioorganic and Medicinal Chemistry, 2008, 16, 14, 7039-7045
- Pergamon-Elsevier Science Ltd, Oxford