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An indole alkaloid with aspidospemane structure possessing a potential antiplasmodial activity,<br />vincadifformine, has been isolated from Aspidosperma pyrifolium Mart. Moreover, 10 derivatives were prepared<br />from the vincadifformine. The study was conducted to evaluate the in vitro antiplasmodial and cytotoxic activity of<br />the vincadifformine and their semisynthetic derivatives. The in vitro antiplasmodial activity was evaluated on<br />Plasmodium falciparum chloroquine-resistant (FcM ) and &ndash;sensitive (Nigerian) strains after 24-h and 72-h incubation, 29<br />while cytotoxic activity was estimated on Hela cells and Cytotoxicity Index (CI = IC on HeLa cells/IC on FcM strain) 50 50 29<br />was calculated to evaluate the safety of tested compounds. Experiment results showed that two compounds (4 and 8)<br />exhibited good antiplasmodial activities in comparison with parent compound, vincadifformine and other tested<br />compounds with IC ranging from 5.3 to 12.8 &mu;M on FcM strain and 11.4 to 24.0 &mu;M on Nigerian strain. In addition, 50 29<br />the CI of two compounds were also lower after 24-h incubation (CI, 2.0 and 4.8) than that of after 72-h incubation (CI,<br />9.5 and 11.5). Further study will be conducted to evaluate quantitative structure-activity relationship (QSAR) in order<br />to design new antimalarial drugs.<br />Keywords : vincadifformine - antiplasmodial &ndash; Plasmodium falciparum &ndash; cytotoxic - HeLa