Organometallic gold(III) complexes with hybrid SNS-donating thiosemicarbazone ligands: cytotoxicity and anti-Trypanosoma cruzi activity

作者: PI da S Maia , ZA Carneiro , CD Lopes , CG Oliveira , João Santana da Silva

DOI: 10.1039/C6DT04307K

关键词:

摘要: Stable organogold(III) compounds of the composition [AuIII(Hdamp)(L1)]Cl are formed from reactions [AuCl2(damp)] with H2L1 (damp− = dimethylaminomethylphenyl; N′-(diethylcarbamothioyl)benzimidothiosemicarbazides). The cationic complexes can be neutralized by weak bases under formation [AuIII(damp)(L1)] compounds. structures products show interesting features like relatively short Au⋯H contacts between methylene protons Hdamp ligand and gold(III) ions. Preliminary biological studies on uncoordinated their gold indicate considerable cytotoxicity for against MCF-7 cells. in vitro trypanocidal activity was evaluated intracellular form Trypanosoma cruzi. organometallic display a remarkable activity, which is dependent alkyl substituents thiosemicarbazone building blocks ligands. One representative complexes, where contains dimethylthiosemicarbazide block, shows amastigote same order magnitude as that standard drug benznidazole. Furthermore, no appreciable toxicity to mice spleen cells observed this compound resulting therapeutic index about 30, strongly recommends it promising candidate development future antiparasitic drug.

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