New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: potential anti-trypanosomal agents

作者:Demoro Bruno; Sarniguet Cynthia; Sanchez Delgado Roberto; Rossi Miriam; Liebowitz Daniel; Caruso Francesco; Olea Azar Claudio; Moreno Virtudes; Medeiros Andrea; Comini Marcelo A; Otero Lucia*; Gambino Dinorah
来源:Dalton Transactions, 2012, 41(5): 1534-1543.
DOI:10.1039/c1dt11519g

摘要

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 PF6, 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.

  • 出版日期2012