Antitumor activity of water-soluble platinum(II) complexes of 1,2-cyclohexanediamine isomers.

Dichloroplatinum(II) complexes of 1,2-cyclohexanediamine isomers were reported to have high antitumor activity against leukemia L-1210 and P-388, but they were hardly soluble in water and, therefore, dibromo- and diiodo-platinum(II) complexes of 1,2-cyclohexanediamine isomers were prepared. They were not soluble in water but showed high antitumor activity. When the chloride ions are replaced with sulfate ions, they become soluble and also they are anti-tumor active. Bismonobromoacetatoplatinum (II) complexes were synthesized and tested. Mono- and bis-(D-glucuronato)platinum(II) complexes of 1,2-cyclohexanediamine isomers were newly synthesized. All of them were freely soluble in water and showed high antitumor activity with low toxicity. The chelated mono(D-glucuronato)platinum(II) was found to be more effective than the monodentate bis(D-glucuronato)platinum (II) complexes.