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A series of Pt(II) complexes trans‐[Pt(PPh2allyl)2(κ1‐S‐SR)2], 1, PPh2allyl=allyldiphenylphosphine, SR=pyridine‐2‐thiol (Spy, 1 a), 5‐(trifluoromethyl)‐pyridine‐2‐thiol (SpyCF3‐5, 1 b), pyrimidine‐2‐thiol (SpyN, 1 c), benzothiazole‐2‐thiol (Sbt, 1 d), benzimidazole‐2‐thiol (Sbi, 1 e), were synthesized. They were characterized by NMR, HR ESI‐MS, and X‐ray crystallography. Treatment of human cancer cell lines (A549, SKOV3, MCF‐7) with these complexes resulted in promising antitumor effects in comparison with cisplatin. These compounds showed suitable selectivity between tumorigenic and non‐tumorigenic (MCF‐10 A) cell lines. Analyses of cell cycle progression and apoptosis were conducted for 1 a, the most cytotoxic compound, to screen dose/time response and to study the antiproliferative mechanism. An electrophoresis mobility shift assay was performed to assess the direct interaction of 1 a with DNA and the strong genotoxic ability was indicated through the comet assay method.

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