Antitumor activity of platinum(II) complexes of 1,2-diamino-cyclohexane isomers

Abstract

Dichloro, dibromo, oxalato, malonato, dinitrato, sulfato and mono and bis-(D-glucuronato) platinum(II) complexes of 1,2-diaminocyclohexane (dach) isomers were prepared and tested on L1210 mouse leukemia employing the NCI protocol for evaluation of Pt analogs. A large number of long-term survivors were observed with certain analogs, though the therapeutic indices (optimal dose/minimum effective dose) were not large. Among the analogs tested, the oxalato, malonato, dinitrato and mono-(D-glucuronato) Pt(II) complexes of trans-1,2-diaminocyclohexane were found to be particularly effective. The glucuronato Pt complexes appear to be promising candidates for clinical trial since they have the highest solubility in water.