RESUMO

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.

Assuntos

Antimaláricos/farmacologia , Complexos de Coordenação/síntese química , Compostos Ferrosos/farmacologia , Compostos Organometálicos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Rutênio/farmacologia , Animais , Antimaláricos/síntese química , Linhagem Celular , Cromatografia em Camada Fina , Complexos de Coordenação/farmacologia , Citotoxinas/farmacologia , Compostos Ferrosos/síntese química , Haplorrinos , Células Hep G2/parasitologia , Humanos , Técnicas In Vitro , Concentração Inibidora 50 , Compostos Organometálicos/síntese química , Rutênio/química , Tamoxifeno/química