Nine platinum(II) complexes with N-monoalkyl 1R, 2R-DACH derivatives as carrier ligands and demethyl-cantharidate as a leaving group were synthesized and spectrally characterized. All the complexes showed considerable cytotoxicity against tested human cancer cell lines: A549, HCT116 HepG-2 and MCF7 cell lines. Especially, complex 2 exhibited potent cytotoxicity against A549 (1.01 mu M) and HCT116 (0.83 mu M) cell lines, and showed no cross-resistance to cisplatin against SGC7901/CDDP cell line (RF = 1.44). In addition, the typical compounds were further studied by flow cytometric analysis and western blot method. The results indicated that they induced apoptosis by a mitochondrial-dependent pathway, which were similar to cisplatin. (C) 2017 Elsevier B.V. All rights reserved.