Summary. The syntheses of dichlorobis(cycloalkylamine)platinum(II) complexes with cis and transcycloalkytamine ligands 2 to cis-PtC12(CaHlsNH2)2 (3-8) and trans-PtC12-(CTH13NH2)2 (9) and trans-PtC12(CsH~sNH2)2 (10)] are described. The distinction between cis and trans isomers was achieved by ~H-NMR spectroscopy. The antitumor activity was determined on the cell proliferation of the human MDA-MB-231 breast cancer ceil line during long-term drug exposure. The complexes with small cycloalkylamine ligands (3-6) were inferior, those with large cycloalkylamine ligands were comparable (7) or superior (8) to cisplatin. Surprisingly, the cis/trans isomers 7/9 and 8/10 were equally active. All cycloalkylamine ligands were inactive. IR-spectroscopic studies showed that the size of the cycloalkylamine ring does not lead to significant differences in the Pt-C1 binding strength. Therefore it is assumed that the markedly stronger antitumor activity of the higher homologues, 7-10, is not the result of a faster reaction with bionucleophils such as DNA. A possible explanation of the high activity of 7-10 is the strong lipophilicity of the complexes. This assumption was confirmed by toxicity tests against confluent cultures.
Keywords. cis-and trans-Dichlorobis(cycloalkylamine)platinum(II)complexes