4.7 Article

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

Journal

DALTON TRANSACTIONS
Volume 41, Issue 5, Pages 1534-1543

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c1dt11519g

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Funding

  1. US National Science Foundation [0521237]
  2. NIH [SC1GM089558-01A1]

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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.

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