Synthesis of Platinum Complexes of 2-Aminoalkylpyridine as Carrier Ligand and Their Antitumor Activities

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Abstract
Platinum complexes of 2-aminoalkylpyridine as a carrier ligand were synthesized and evaluated for antitumor activities against P388 leukemia in mice. Among the analogues, (2-aminomethylpyridine)oxalatoplatinum (II) (X-1), (2-aminomethylpyridine)malonatoplatinum (II), (X-2), (2-aminomethylpyridine)(1,1-cyclobutanedicarboxylato)platinum (II) (X-3), (2-(1-aminoethyl)pyridine)oxalatoplatinum (II) (X-12) and (2-(1-aminopropyl)pyridine)oxalatoplatinum (II) (X-17) exhibited excellent activity and were comparable to cis-diamminedichloroplatinum (II) and superior to (1,1-cyclobutanedicarboxylato)diammineplatinum (II). Structure-activity relationships are discussed.