PREPARATION AND ANTI-TUMOR EVALUATION OF WATER-SOLUBLE DERIVATIVES OF DICHLORO(1,2-DIAMINOCYCLOHEXANE)PLATINUM(II)

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  • 1 January 1977
    • journal article
    • research article
    • Vol. 61  (8) , 1519-1525
Abstract
The structure of the antitumor agent, dichloro(1,2-diaminocyclohexane)platinum(II) (NSC-194814), was modified by replacing the chlorides with organic or inorganic anions. Eighteen new Pt complex were so isolated and their antitumor properties against the L1210 leukemia in C57BL/6 .times. DBA/2 mice were evaluated. Most of the complexes were readily soluble in water and some had enhanced antitumor activity compared to the parent dichloro complex. Increased solubility with retention of significant antitumor activity was obtained by oxidizing the parent dichloroplatinum(II) complex with halogen or peroxide to give 2 Pt(IV) complexes. Some previously reported Pt complexes with P, Se, or Te electron donor ligands were also synthesized and assessed for antitumor action, but these did not show appreciable activity.