Synthesis and biological evaluation of novel dinuclear platinum(II) complexes derived from a novel chiral ligand

Abstract

As the carrier group, six novel dinuclear platinum(II) complexes with a tetradentate ligand, (1R,1′R,2R,2′R)-N1,N1′-(1,2-phenylenebis(methylene))dicyclohexane-1,2-diamine (HL), have been designed, synthesized and characterized. To characterize the intermediate [Pt2I4L] and compounds A1–A6 IR, 1H NMR and ESI-MS spectroscopies and element analysis were applied. The newly synthesized compounds possessed DNA unwinding capability similar to cisplatin by the means of agarose gel electrophoresis. In addition, the evaluation of these metal complexes in vitro cytotoxicities against HepG-2, A549, HCT-116 and MCF-7 cell lines were conducted by MTT assay. According to the results, all targeted complexes exhibited antitumor activity against HEPG-2, A549 and HCT-116 cell lines. Compound A2 showed better cytotoxicity than carboplatin against HepG-2 and A549 cell lines and also presented a certain activity against HCT-116 which are insensitive to carboplatin. The anticancer activity of Compound A1 was similar to carboplatin on HepG-2 and A549 cell lines.