Novel mononuclear complexes of Pt(II), cis-[PtCl2(DMSO) HL]center dot 2DMSO (1), where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5-a] pyrimidine-6-carboxylic acid and Pt(bdt)Cl-2 (2), where bdt = [2,4-bis(5,6-diphenyl-1,2,4-triazin-3yl)-pyridine] have been synthesized and characterized by elemental analysis, IR and H-1 NMR spectroscopy and X-ray crystallography diffraction analyses. The molecular structure of (1) shows that Pt(II) ion has a square planar geometry with N(3) bonded heterocycle ligand, two cis chloride anions and S-bonded dimethylsulfoxide. The antiproliferative activity of complexes (1) and (2) has been tested in vitro against HepG2 human hepatoma cells and non-malignant human-derived hepatic cells (Chang). Complex (1), cis-[PtCl2(DMSO) HL]center dot 2DMSO, was effective inducer of apoptotic death on HepG2 cells and its cytotoxic activity was higher than that exerted by cisplatin. Apoptosis effect was associated with externalization of plasma membrane phosphatidylserine. (C) 2014 Elsevier B. V. All rights reserved.