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ANTITUMORAL, ANTILEISHMANIAL AND ANTIMALARIAL ACTIVITY OF PENTACYCLIC 1,4-NAPHTHOQUINONE DERIVATIVES
Antiparasitic
Pterocarpans
Naphtoquinones
Oxa-Heck reaction
Antimalarial
Leishmanicide
Author
Affilliation
Abstract in Portuguese
As pterocarpanquinonas 8a-c, previamente sintetizadas em nosso laboratório, e uma série homóloga de derivados, substâncias 9a-c preparadas neste trabalho, foram avaliadas em células de câncer de mama (MCF-7) e em cultura dos parasitas Leishmania amazonensis e Plasmodium falciparum. As substâncias 8a-c foram mais potentes que 9a-c nas células tumorais e em Leishmania amazonensis. Por outro lado, 9a-c mostraram ser as mais ativas sobre o Plasmodium falciparum. Todas as substâncias estudadas foram biosseletivas, apresentando baixa citotoxicidade para linfócitos murinos frescos e linfócitos humanos ativados pelo mitógeno fitoemoaglutinina (PHA).
Abstract
Pterocarpanquinones 8a-c, previously synthesized in our laboratory, and an homologous series of derivatives, compounds 9a-c prepared in this work, were evaluated on breast cancer cells (MCF-7) and on the parasites Leishmania amazonensis and Plasmodium falciparum, in culture. Compounds 8a-c were more potent than 9a-c on tumor cells and Leishmania amazonensis. On the other hand, 9a-c showed to be more active on Plasmodium falciparum. All the compounds studied were bioselective, presenting negligible cytotoxicity against fresh murine lymphocytes and human lymphocytes activated by the mitogen phytohemaglutinin (PHA).
Keywords
AntineoplasicAntiparasitic
Pterocarpans
Naphtoquinones
Oxa-Heck reaction
Antimalarial
Leishmanicide
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