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: Bruno Demoro, Cynthia Sarniguet, Roberto Sánchez-Delgado, Miriam Rossi, Daniel Liebowitz, Francesco Caruso, Claudio Olea-Azar, Virtudes Moreno, Andrea Medeiros, Marcelo A Comini, Lucía Otero, Dinorah Gambino
• Journal: Dalton transactions (Cambridge, England : 2003) (Dalton Trans) Vol. 41 Issue 5 Pg. 1534-43 (Feb 07 2012) ISSN: 1477-9234 [Electronic] England
• PMID: 22138896 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.)

Chemical References

• Ligands
• Organoselenium Compounds
• Trypanocidal Agents
• DNA
• calf thymus DNA

Topics

• Animals
• Cattle
• Cell Line
• Crystallography, X-Ray
• DNA (metabolism)
• Humans
• Ligands
• Macrophages (drug effects)
• Mice
• Models, Molecular
• Organoselenium Compounds (chemistry, pharmacology)
• Trypanocidal Agents (chemistry, pharmacology)
• Trypanosoma brucei brucei (drug effects)
• Trypanosomiasis, African (drug therapy)