Syntheses and Antitumor Activities of 1R,2R-Cyclohexanediamine Pt(II) Complexes Containing Dicarboxylates(Medicinal Chemistry,Chemical)

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New 1R,2R-cyclohexanedimine(=1R,2R-dach) Pt(II) complexes containing dicarboxylate ions. i.e., ketomalonate, malate. saccharate, glutarate, diphenate, and α,β-diphenylsuecinate were synthesized and tested against leukemia L1210 in vivo. All of the dicarboxylato Pt(II) complexes showed relatively high antitumor activities with T/C% values of more than 200 at optimal doses. In particular, mucato and α,β-diphenylsuecinato Pt(II) complexes exhibited excellent antitumor activities with T/C% values of 348 and 369, respectively, with 3 cured mice out of six. The dicarboxylato Pt(II) complexes were determined by elemental analyses to contatin dicarboxylates : Pt : 1R,2R-dach in a ratio of 1:1:1. The molecular secondary ion mass spectra of saecharato and glutarato Pt(II) complexes indicate that these complexes exist in a binuclear form together with a mononuclear form in aqucous solution.
社団法人日本薬学会の論文
1987-01-25