Aspartato(1,2-cyclohexanediamine)platinum(II) complexes: synthesis and characterization; effects of minor impurities on antitumor activity

Abstract

Aspartato(1,2-cyclohexanediamine)platinum(II) (ADP), where 1,2-cyclohexanediamine (DAC) is either trans-RR-, trans-SS-, meso-RS-, or a mixture of the three isomers (ADP mixture), has been synthesized and evaluated for antitumor activity. The structures of the complexes have been characterized by various spectroscopic techniques (IR, 1H, 13C, 195Pt and 2D-COSY (1H{1H}) and 2D-HETCOSY (1H{13C}) NMR). Purification and murine antitumor activity of the individual ADP isomers indicate that minor impurities in the ADP mixture have a significant effect on the potency of the platinum complexes.