Antitumor activity of platinum(II) complexes of 1,2-diamino-cyclohexane isomers.
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.
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D007939:Leukemia L1210 / Q000188:drug therapy; D008297:Male; D051379:Mice; D009944:Organoplatinum Compounds / Q000627:therapeutic use* / Q000633:toxicity; D000077150:Oxaliplatin; D012995:Solubility; D013237:Stereoisomerism
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C030109:platinum(II) dibromo-1,2-diaminocyclohexane; D000077150:Oxaliplatin; C011076:platinum(II) 1,2-diaminocyclohexane malonate; C013933:dichloro-1,2-diaminocyclohexane platinum complex; C012936:1,2-cyclohexanediamine dinitratoplatinum; C024236:1,2-diaminocyclohexyl platinum sulfate; C030111:platinum(II) 1,2-diaminocyclohexane glucuronate; C030112:platinum(II) 1,2-diaminocyclohexane bis(glucuronate)