SYNTHESIS AND ANTITUMOR-ACTIVITY OF (DIAMINE)PLATINUM(II) COMPLEXES OF BENZYLMALONATE DERIVATIVES

(Diamine)platinum(II) complexes of benzylmalonate derivatives as a lea ving group designed in a wide range of lipophilicity and water-solubil ity were prepared and their antitumor activities were attempted to cor relate to their lipophilicity or solubility. a good relationship was o bserved between their in vitro toxicity and solubility of the title co mplexes with the same carrier ligand, DACH (trans-(+/-)-1,2-diaminocyc lohexane): The most soluble complexes are most cytoxic whereas the lea st soluble complexes are least cytotoxic. However, no relationship cou ld be established between their in vivo activity and their lipophilici ty or solubility presumably due to other pharmacokinetic factors invol ved in vivo. The molecular structure of (IPA)(2)Pt(DBM). 2CH(3)OH (IPA = isopropylamine; DBM = dibenzylmalonate) was determined by X-ray dif fraction: space group P2(1)/n, a = 11.433 (3), b = 14.461 (4), c = 17. 478 (4) Angstrom, beta = 97.25 (3)degrees, z = 4, R = 0.0437. (C) 1997 Elsevier Science Inc.