Thiophene-2-carbaldehyde N(4)-cyclohexylthiosemicarbazone C 12 H 17 N 3 S 2 (HL) and diorganotin(IV) complex [Ph 2 Sn(L)Cl] (1) have been synthesized and characterized by elemental analysis, IR, and single-crystal X-ray diffraction. Complex 1 contains mononuclear neutral molecule composed of one five-coordinated diorganotin(IV) ion, one NS bidentate anionic thiosemicarbazone ligand, one chloridion, and two phenyl group, respectively. In vitro biological studies have indicated that coupling of HL with Ph 2 Sn (IV) leads to an enhancement of the cytotoxicity of the free ligand. Importantly, complex 1 could distinguish the human liver hepatocellular carcinoma HepG-2 cells from normal hepatocyte QSG7701 cells.