Synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
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Authors: | Whittell Louise R Batty Kevin T Wong Rina P M Bolitho Erin M Fox Simon A Davis Timothy M E Murray Paul E |
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Affiliation: | School of Pharmacy, Curtin University, Bentley, GPO Box U1987, Perth, Western Australia 6845, Australia. |
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Abstract: | A series of mono- and di-substituted analogues of isocryptolepine have been synthesized and evaluated for in vitro antimalarial activity against chloroquine sensitive (3D7) and resistant (W2mef) Plasmodium falciparum and for cytotoxicity (3T3 cells). Di-halogenated compounds were the most potent derivatives and 8-bromo-2-chloroisocryptolepine displayed the highest selectivity index (106; the ratio of cytotoxicity (IC(50)=9005 nM) to antimalarial activity (IC(50)=85 nM)). Our evaluation of novel isocryptolepine compounds has demonstrated that di-halogenated derivatives are promising antimalarial lead compounds. |
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