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Type: Artigo de periódico
Title: Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog
Author: Montoia, A
Silva, LFRE
Torres, ZE
Costa, DS
Henrique, MC
Lima, ES
Vasconcellos, MC
Souza, RCZ
Costa, MRF
Grafov, A
Grafova, I
Eberlin, MN
Tadei, WP
Amorim, RCN
Pohlit, AM
Abstract: 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.
Subject: 2-Methyl-1,2,3,4-tetrahydroellipticine
Plasmodium falciparum
Country: Inglaterra
Editor: Pergamon-elsevier Science Ltd
Citation: Bioorganic & Medicinal Chemistry Letters. Pergamon-elsevier Science Ltd, v. 24, n. 12, n. 2631, n. 2634, 2014.
Rights: fechado
Identifier DOI: 10.1016/j.bmcl.2014.04.070
Date Issue: 2014
Appears in Collections:Unicamp - Artigos e Outros Documentos

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