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Mem. Inst. Oswaldo Cruz ; 110(8): 981-988, Dec. 2015. tab, graf
Article de Anglais | LILACS | ID: lil-769827

RÉSUMÉ

This work reports the in vitro activity against Plasmodium falciparumblood 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.


Sujet(s)
Animaux , Humains , Antipaludiques/pharmacologie , Complexes de coordination/synthèse chimique , Composés du fer II/pharmacologie , Composés organométalliques/pharmacologie , Plasmodium falciparum/effets des médicaments et des substances chimiques , Ruthénium/pharmacologie , Antipaludiques/synthèse chimique , Lignée cellulaire , Chromatographie sur couche mince , Complexes de coordination/pharmacologie , Cytotoxines/pharmacologie , Composés du fer II/synthèse chimique , Haplorhini , /parasitologie , Techniques in vitro , Composés organométalliques/synthèse chimique , Ruthénium/composition chimique , Tamoxifène/composition chimique
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