期刊
MEMORIAS DO INSTITUTO OSWALDO CRUZ
卷 110, 期 8, 页码 981-988出版社
FUNDACO OSWALDO CRUZ
DOI: 10.1590/0074-02760150163
关键词
Plasmodium falciparum; metallodrug activity; ruthenocifens; ferrocifens
资金
- CNPq/FAPEMIG
- FAPEAL/CNPq
- CAPES
- MS
- CNPq
- MCT/CNPq/CT-Saude/MS/SCTIE/DECIT [PRONEX-55675/2009-2, Doencas Negligenciadas-404455/2012-3]
- FAPEMIG [PRONEX-16712]
- ANR (Mecaferrol) [ANR-10-BLAN-706]
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.
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