Structures of Platinum(II) Complexes of 2-Aminomethylaziridine and S-2-Aminomethylazetidine and Correlation of Anticancer Activities of (2-Aminomethylazacycioalkane)platinum(II) Complexes with the Geometry of the Chelate Rings Formed with Platinum(II)

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The spectroscopic properties of platinum(II) complexes with 2-aminomethyl-derivatives of small-membered 1-aza-cycloalkane, i.e., =2-aminomethylaziridine = azida and S-2-aminoinethylazetidine =S-azeda, and the crystal structures of their dichloro complexes demonstrate that the conformation of the fused three- (azida) or four- (S-azeda) and five-membered chelate ring formed by the coordination of S-azida and S-azeda to platinum(II) has an S(N) absolute configuration at the secondary amine site and that the two alkyl groups extend axially from the five-membered chelate ring. The chelate ring of the azida is more planar than the S-azeda or other 2-aminomethyl-1-azacycloalkanes. The anticancer activity reported for azeda and 2-aminomethylpyrrolidine appears to be related to their coordination structure, namely the presence of cis-fused successive rings.
公益社団法人日本薬学会の論文
2004-01-01