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

Abstract

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, 1H 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)8COO– as the leaving groups, respectively, gave better antitumor activity than carboplatin against HepG-2 and A549 cell lines.