Antitumoral, Antileishmanial and Antimalarial Activity of Pentacyclic 1,4-Naphthoquinone Derivatives

被引:91
作者
da Silva, Alcides J. M. [1 ]
Netto, Chaquip D. [1 ]
Pacienza-Lima, Wallace [2 ]
Torres-Santos, Eduardo Caio [2 ,3 ]
Rossi-Bergmann, Bartira [2 ]
Maurel, Severine [4 ]
Valentin, Alexis [4 ]
Costa, Paulo R. R. [1 ]
机构
[1] Univ Fed Rio de Janeiro, Ctr Ciencias Saude, Lab Quim Bioorgan, BR-21941590 Rio De Janeiro, Brazil
[2] Univ Fed Rio de Janeiro, Ctr Ciencias Saude, Inst Biofis Carlos Chagas Filho, BR-21941590 Rio De Janeiro, Brazil
[3] Inst Oswaldo Cruz, Lab Bioquim Tripanosomatideos, BR-21045900 Rio De Janeiro, Brazil
[4] Univ Toulouse 3, Fac Pharm, IRD, UMR 152, F-31062 Toulouse 4, France
关键词
antineoplasic; antiparasitic; pterocarpans; naphtoquinones; oxa-Heck reaction; antimalarial; leishmanicide; CATECHOL ORTHO-QUINONES; BETA-LAPACHONE; PHARMACOLOGICAL EVALUATION; REGIOSELECTIVE SYNTHESIS; RADICAL CYCLIZATION; HECK OXYARYLATION; IN-VITRO; PTEROCARPANS; CANCER; ISOFLAVONOIDS;
D O I
10.1590/S0103-50532009000100026
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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).
引用
收藏
页码:176 / U222
页数:13
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