Abstract
Nine platinum(II) complexes with N-monoalkyl 1R,2R-DACH derivatives as carrier ligands and demethylcantharidate 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 (1.01μM) and HCT116 (0.83μM) 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.
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