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有机锡化合物抗肿瘤活性的研究。I. 二有机锡二卤化物和二拟卤化物配合物。

Investigations into the antitumour activity of organotin compounds. I. Diorganotin dihalide and di-pseudohalide complexes.

作者信息

Crowe A J, Smith P J, Atassi G

出版信息

Chem Biol Interact. 1980 Oct;32(1-2):171-8. doi: 10.1016/0009-2797(80)90075-7.

Abstract

The antitumor activity of a series of diorganotin dihalide and di-pseudohalide complexes, R2SnX2, L2, where R = Methyl (Me), Ethyl (Et), n-Propyl (Pr), n-Butyl (Bu) or Phenyl (Ph); X = F, Cl, Br, I or NCS; and L = O- or N- donor organic ligand, which were modelled on the active platinum complexes, has been investigated. A number of these derivatives exhibit reproducible therapeutic activity in vivo towards P-388 lymphocytic leukaemia in mice, particularly the diethyltin dihalide and dipseudohalide complexes. The possible factors influencing activity are discussed, both in terms of the stereochemistry of the dialkyltin compounds and their structural similarity to the platinum antitumour drugs.

摘要

一系列二有机锡二卤化物和二拟卤化物配合物R2SnX2、L2的抗肿瘤活性已被研究,其中R = 甲基(Me)、乙基(Et)、正丙基(Pr)、正丁基(Bu)或苯基(Ph);X = F、Cl、Br、I或NCS;L = O或N供体有机配体,这些配合物是以活性铂配合物为模型设计的。其中许多衍生物在体内对小鼠P - 388淋巴细胞白血病表现出可重复的治疗活性,特别是二乙基锡二卤化物和二拟卤化物配合物。从二烷基锡化合物的立体化学及其与铂抗肿瘤药物的结构相似性两方面讨论了影响活性的可能因素。

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