Synthesis, characterization, crystal structure and antiproliferative activity of platinum(II) complexes with 2-acetylpyridine-4-cyclohexyl-thiosemicarbazone

Abstract New platinum complexes have been synthesized by the reaction of Na 2 PtCl 4 with 2-acetylpyridine-4-cyclohexyl-thiosemicarbazone, HAc4CyclHexyl ( 1 ). The new complexes [Pt(Ac4CyclHexyl)Cl] ( 2 ) and [Pt(Ac4CyclHexyl) 2 ] ( 3 ) have been characterized by elemental analyses and spectroscopic studies. The crystal structure of the complex [Pt(Ac4CyclHexyl)Cl] · DMF has been solved by single-crystal X-ray diffraction. The anion of Ac4CyclHexyl coordinates in a planar conformation to the central platinum(II) through the pyridyl N, azomethine N and thiolato S atoms. The crystal packing is determined by double intermolecular hydrogen interactions, π–π, Pt–C and Pt–π contacts. The cytotoxic activities of 1 – 3 have been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines: MCF-7 (human breast cancer cell line), T24 (bladder cancer cell line), A-549 (non-small cell lung carcinoma) and a mouse L-929 (a fibroblast-like cell line cloned from strain L). The compounds 1 – 3 display IC 50 values in a μM range better than that of the antitumor drug cisplatin and are considered as agents with potential antitumor activity candidates for further stages of screening in vitro and/or in vivo.