title: Antiplasmodial activity of iron(II) and ruthenium(II) organometallic complexes against Plasmodium falciparum blood parasites.
abstract: 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.
authors.affiliation: Centro de Pesquisas René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, MG, Brasil.
authors.forename: Nicolli Bellotti de
authors.initials: NB
authors.lastname: Souza
authors.affiliation: Centro de Pesquisas René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, MG, Brasil.
authors.forename: Anna Caroline Campos
authors.initials: AC
authors.lastname: Aguiar
authors.affiliation: Instituto de Química e Biotecnologia, Universidade Federal de Alagoas, Maceió, AL, Brasil.
authors.forename: Alane Cabral de
authors.initials: AC
authors.lastname: Oliveira
authors.affiliation: Université Pierre-et-Marie-Curie, Sorbonne Universités, Paris, France.
authors.forename: Siden
authors.initials: S
authors.lastname: Top
authors.affiliation: Université Pierre-et-Marie-Curie, Sorbonne Universités, Paris, France.
authors.forename: Pascal
authors.initials: P
authors.lastname: Pigeon
authors.affiliation: Université Pierre-et-Marie-Curie, Sorbonne Universités, Paris, France.
authors.forename: Gérard
authors.initials: G
authors.lastname: Jaouen
authors.affiliation: Instituto de Química e Biotecnologia, Universidade Federal de Alagoas, Maceió, AL, Brasil.
authors.forename: Marilia Oliveira Fonseca
authors.initials: MO
authors.lastname: Goulart
authors.affiliation: Centro de Pesquisas René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, MG, Brasil.
authors.forename: Antoniana Ursine
authors.initials: AU
authors.lastname: Krettli
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D002855:Chromatography, Thin Layer; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D003603:Cytotoxins / Q000494:pharmacology; D005296:Ferrous Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D000882:Haplorhini; D056945:Hep G2 Cells / Q000469:parasitology; D006801:Humans; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*; D012428:Ruthenium / Q000737:chemistry / Q000494:pharmacology*; D013629:Tamoxifen / Q000737:chemistry
chemical_list: D000962:Antimalarials; D056831:Coordination Complexes; D003603:Cytotoxins; D005296:Ferrous Compounds; D009942:Organometallic Compounds; C514120:ferrocifen; D013629:Tamoxifen; D012428:Ruthenium