Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Ellipticine has been shown previously to exhibit excellent in vitro antiplasmodial activity and in vivo antimalarial properties that are comparable to those of the control drug chloroquine in a mouse malaria model. Ellipticine derivatives and analogs exhibit antimalarial potential however only a few have been studied to date. Herein, ellipticine and a structural analog were isolated from Aspidosperma vargasii bark. A-ring brominated and nitrated ellipticine derivatives exhibit good in vitro inhibition of Plasmodium falciparum K1 and 3D7 strains. Several of the compounds were found not to be toxic to human fetal lung fibroblasts. 9-Nitroellipticine (IC50 = 0.55 mu M) exhibits greater antiplasmodial activity than ellipticine. These results are further evidence of the antimalarial potential of ellipticine derivatives. (C) 2014 Elsevier Ltd. All rights reserved.241226312634Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)National Malaria Network, Bionorth NetworkAmazonas State Foundation for the Advancement of Research (FAPEAM/PRONEX)European Community FP7-Marie Curie Actions-People-International Research Staff Exchange Scheme (IRSES)PIRSES-GA-2011-295262Academy of Finland and Magnus Ehrnrooth FoundationConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq