Antitumor platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with dicarboxylates as leaving groups

Abstract

Four platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with different bidentate dicarboxylates (1 oxalate, 2 malonate, 3 1,1-cyclobutanedicarboxylate and 4 3-hydroxy-1,1-cyclobutanedicarboxylate) as leaving groups were synthesized and characterized by elemental analyses, IR and 1HNMR spectra together with ESI-MS spectroscopy. All complexes showed considerable cytotoxicity against the tested four human tumor cell lines including A549, HCT-116, HepG-2 and MCF-7. Especially, complex 4 showed good cytotoxicity against A549 (IC50=3.5μM) and HCT-116 (IC50=0.9μM) cancer cell lines. Moreover, complex 3 is the most effective agent among the tested compounds against MCF-7 cell line (IC50=1.1μM). The DNA binding behavior of both complexes 3 and 4, studied by agarose gel electrophoresis, revealed that they bound to DNA in almost the same way as cisplatin.