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[紫杉烷类化合物的精细立体结构研究]

[Studies on the fine stereostructure of taxoids].

作者信息

Wu N, Lu Y, Zheng Q, Fang W, Gao Y, Fang Q, Zhou T

机构信息

Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.

出版信息

Yao Xue Xue Bao. 1998 Oct;33(10):759-63.

Abstract

The anticancer drug taxol is a new type antimicrotubular drug. The structure-activity relationship study on taxol and its analogs has indicated the importance of the C13 side chain and the C4-C5-C20 epoxypropane group. The crystal structures of 4 taxoids having the basic skeleton with 5/7/6 membered ring and three types of 10 taxoids having the basic skeleton with 6/8/6 membered ring have been analyzed. The effects of the induction by different substructures at C4 on the stereostructures of taxoids were studied, and the relationship between the 6/8/6/4 skeleton and the anticancer activity was discussed from the crystallographic point.

摘要

抗癌药物紫杉醇是一种新型抗微管药物。对紫杉醇及其类似物的构效关系研究表明了C13侧链和C4-C5-C20环氧丙烷基团的重要性。已分析了具有5/7/6元环基本骨架的4种类紫杉醇的晶体结构以及具有6/8/6元环基本骨架的3种类型10种类紫杉醇的晶体结构。研究了C4处不同亚结构的诱导对类紫杉醇立体结构的影响,并从晶体学角度讨论了6/8/6/4骨架与抗癌活性之间的关系。

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