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

• Main Authors: Nicolli Bellotti de Souza, Anna Caroline Campos Aguiar, Alane Cabral de Oliveira, Siden Top, Pascal Pigeon, Gérard Jaouen, Marilia Oliveira Fonseca Goulart, Antoniana Ursine Krettli
• Format: Article
• Language: English
• Published: Instituto Oswaldo Cruz, Ministério da Saúde 2015-01-01
• Series: Memórias do Instituto Oswaldo Cruz.
• Subjects: Plasmodium falciparum; metallodrug activity; ruthenocifens; ferrocifens
• Online Access: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762015005025102&lng=en&tlng=en
• ISSN: 1678-8060

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.