title: New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: potential anti-trypanosomal agents.
abstract: In the search for new therapeutic tools against neglected diseases produced by trypanosomatid parasites, and particularly against African Trypanosomiasis, whose etiological agent is Trypanosoma brucei, organoruthenium compounds with bioactive nitrofuran containing thiosemicarbazones (L) as co-ligands were obtained. Four ruthenium(II) complexes with the formula [Ru(2)(p-cymene)(2)(L)(2)]X(2), where X = Cl or PF(6), were synthesized and the crystal structures of two of them were solved by X-ray diffraction methods. Two of the complexes show significant in vitro growth inhibition activity against Trypanosoma brucei brucei and are highly selective towards trypanosomal cells with respect to mammalian cells (J774 murine macrophages). These promising results make the title organoruthenium compounds good lead candidates for further developments towards potential antitrypanosomal organometallic drugs.
authors.affiliation: Cátedra de Química Inorgánica, Departamento Estrella Campos, Facultad de Química, Universidad de la República (UdelaR), Gral. Flores 2124, 11800, Montevideo, Uruguay.
authors.forename: Bruno
authors.initials: B
authors.lastname: Demoro
authors.forename: Cynthia
authors.initials: C
authors.lastname: Sarniguet
authors.forename: Roberto
authors.initials: R
authors.lastname: Sánchez-Delgado
authors.forename: Miriam
authors.initials: M
authors.lastname: Rossi
authors.forename: Daniel
authors.initials: D
authors.lastname: Liebowitz
authors.forename: Francesco
authors.initials: F
authors.lastname: Caruso
authors.forename: Claudio
authors.initials: C
authors.lastname: Olea-Azar
authors.forename: Virtudes
authors.initials: V
authors.lastname: Moreno
authors.forename: Andrea
authors.initials: A
authors.lastname: Medeiros
authors.forename: Marcelo A
authors.initials: MA
authors.lastname: Comini
authors.forename: Lucía
authors.initials: L
authors.lastname: Otero
authors.forename: Dinorah
authors.initials: D
authors.lastname: Gambino
mesh_terms: D000818:Animals; D002417:Cattle; D002460:Cell Line; D018360:Crystallography, X-Ray; D004247:DNA / Q000378:metabolism; D006801:Humans; D008024:Ligands; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008958:Models, Molecular; D016566:Organoselenium Compounds / Q000737:chemistry* / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects*; D014353:Trypanosomiasis, African / Q000188:drug therapy
chemical_list: D008024:Ligands; D016566:Organoselenium Compounds; D014344:Trypanocidal Agents; D004247:DNA; C427203:calf thymus DNA