Wu N, Lu Y, Zheng Q, Fang W, Gao Y, Fang Q, Zhou T
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.
Yao Xue Xue Bao. 1998 Oct;33(10):759-63.
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.
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。