Diamine platinum complexes as antitumor agents

Abstract

Novel 1,4-diaminocyclohexane platinum II and platinum IV complexes were synthesized which show activity in vivo against tumor models resistant to cis-platin and tetraplatin. The novel complexes include the sulfato, chloro, hydroxyl, acetato methylmalonato, tartronato and 1,1-cyclobutane dicarboxylato as leaving ligands and 1,4-DACH amine as non-leaving ligands. The complexes showed good in vitro cytotoxic activity against murine leukemia L1210/0 and human ovarian A2780 cell lines. High in vivo activity was shown against L1210 leukemia cells and against cis-platin resistant L1210/DDP and tetraplatin resistant L1210/DACH. Excellent antitumor activity against M5076 was also exhibited by the new complexes. Additionally, the platinum complexes did not elicit any indication of nephrotoxicity in the in vivo tests.

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