In vitro biological evaluation of platinum(II) complexes with 1-(methoxy substituted benzyl) azetidine-3,3-dicarboxylato ligands.

Abstract A number of platinum(II) complexes with ammine or 1 R ,2 R -diaminocyclohexane as carrier ligands and 1-(methoxy-substituted benzyl) azetidine-3,3-dicarboxylate as leaving groups were synthesized and spectrally characterized. Biological evaluation in vitro showed that some of compounds showed positive antitumor activity. In particular, complex 3a , (1 R ,2 R -diaminocyclohexane)[1-(3-methoxylbenzyl) azetidine-3,3-dicarboxylato)- O , O ′] platinum(II), possessed a potent antitumor effect comparable to cisplatin and/or oxaliplatin, and very low toxicity in vivo. Preliminary antitumor mechanism of 3a has been investigated by cell apoptosis assays compared with cisplatin and oxaliplatin.