Preparation and in vitro cytotoxicity of oxaliplatin derivatives with chiral amino acid as the carrier group

Novel platinum(II) compounds with a new chiral ligand were designed, prepared and biologically evaluated. Results indicated that compounds P3 and P4 showed better antitumor activity than carboplatin against two selected human cell lines. Eight oxaliplatin derivatives with chiral amino acid, 2-{[(1R, 2R)-2-aminocyclohexyl] amino} propanoic acid, as the carrier group, were designed, synthesized, and spectrally characterized by IR, H-1 NMR, MS spectra, and microanalyses. In vitro cytotoxicities against human HepG-2, MCF-7, A549, and HCT-116 cell lines were evaluated by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazo-liumbromide assay. Results indicated that all compounds exhibited sensitivity to HepG-2 cell line, and among them, compounds P3 and P4 which have CH3(CH2)6COO(-) and CH3(CH2)(8)COO- as the leaving groups, respectively, gave better antitumor activity than carboplatin against HepG-2 and A549 cell lines.