Synthesis, spectroscopic characterization and antiproliferative activity of two platinum(II) complexes containing N-donor heterocycles

• Pt(II) complexes with heterocyclic ligands were synthesized and structural characterized.
• cis-[PtCl2(DMSO)HL]·2DMSO (1), was effective inducer of apoptotic death on HepG2 cells.
• The antiproliferative efficacy of 1 appeared twofold higher than that of cisplatin.

Novel mononuclear complexes of Pt(II), cis-[PtCl2(DMSO)HL]·2DMSO (1), where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylic acid and Pt(bdt)Cl2 (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 1H 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]·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.

The crystal and molecular structure of the compound cis-[PtCl2(DMSO)HL]·2DMSO is reported. The complex was characterized in the solid state and in solution. The antiproliferative activity of complex has been tested in vitro against HepG2 human hepatoma cells and non-malignant human-derived hepatic cells (Chang).Figure optionsDownload as PowerPoint slide