Antiplasmodial activity of iron(II) and ruthenium(II) organometallic complexes against Plasmodium falciparum blood parasites

被引：9
|
作者：
de Souza, Nicolli Bellotti [1 ]
Campos Aguiar, Anna Caroline [1 ]
de Oliveira, Alane Cabral [2 ,3 ]
Top, Siden [4 ]
Pigeon, Pascal [4 ,5 ]
Jaouen, Gerard [4 ,5 ]
Fonseca Goulart, Marilia Oliveira [2 ]
Krettli, Antoniana Ursine [1 ]
机构：
[1] Fundacao Oswaldo Cruz, Ctr Pesquisas Rene Rachou, Belo Horizonte, MG, Brazil
[2] Univ Fed Alagoas, Inst Quim & Biotecnol, Maceio, AL, Brazil
[3] Univ Fed Alagoas, Fac Nutr, Maceio, AL, Brazil
[4] Univ Paris 06, Sorbonne Univ, UMR 8232, Paris, France
[5] Ecole Natl Super Chim Paris, F-75231 Paris 05, France
来源：
MEMORIAS DO INSTITUTO OSWALDO CRUZ | 2015年 / 110卷 / 08期
关键词：
Plasmodium falciparum; metallodrug activity; ruthenocifens; ferrocifens; ESTROGEN-RECEPTOR MODULATORS; IN-VITRO ANTIMALARIAL; ANTIPROLIFERATIVE ACTIVITY; BIOLOGICAL EVALUATION; ARENE COMPLEXES; CELL-GROWTH; BREAST; RESISTANCE; FERROQUINE; OXIDATION;
D O I：
10.1590/0074-02760150163
中图分类号：
R38 [医学寄生虫学]; Q [生物科学];
学科分类号：
07 ; 0710 ; 09 ; 100103 ;
摘要：
This work reports the in vitro activity against Plasmodium falciparum blood forms (W2 clone, chloroquine-resistant) of tamoxifen-based compounds and their ferrocenyl (ferrocifens) and ruthenocenyl (ruthenocifens) derivatives, as well as their cytotoxicity against HepG2 human hepatoma cells. Surprisingly with these series, results indicate that the biological activity of ruthenocifens is better than that of ferrocifens and other tamoxifen-like compounds. The synthesis of a new metal-based compound is also described. It was shown, for the first time, that ruthenocifens are good antiplasmodial prototypes. Further studies will be conducted aiming at a better understanding of their mechanism of action and at obtaining new compounds with better therapeutic profile.
引用
收藏
页码：981 / 988
页数：8
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