期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 12, 页码 2631-2634出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.04.070
关键词
2-Methyl-1,2,3,4-tetrahydroellipticine; 9-Nitroellipticine; 7-Nitroellipticine; 7,9-Dibromoellipticine; Plasmodium falciparum
资金
- Brazilian National Council for Scientific and Technological Development (CNPq)
- National Malaria Network, Bionorth Network
- Amazonas State Foundation for the Advancement of Research (FAPEAM/PRONEX)
- European Community FP7-Marie Curie Actions-People-International Research Staff Exchange Scheme (IRSES)
- PIRSES-GA-2011-295262
- Academy of Finland and Magnus Ehrnrooth Foundation
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.
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