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[源自华蟾素A的新型紫杉烷类化合物的结构修饰及构效关系研究]

[Studies on structure modification and structure-activity relationship of new taxoids derived from sinenxan a].

作者信息

Huang G, Guo J, Liang X

机构信息

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

出版信息

Yao Xue Xue Bao. 1998 Aug;33(8):576-86.

Abstract

In order to develop new taxol analogues with possible antitumor properties, sinenxan A (SIA), a new biosynthetic taxoid, was chemically modified, mainly by esterification of C14-OH with taxol-like side-chain acids. Twenty-one new taxoids thus formed were tested on three kinds of cell lines. Their activities are far below those of taxol. The SAR of SIA derivatives partly agree with that of taxol and can be roughly discerned.

摘要

为了开发具有潜在抗肿瘤特性的新型紫杉醇类似物,对一种新的生物合成紫杉烷类化合物——中国红豆杉素A(SIA)进行了化学修饰,主要是将C14-OH与类似紫杉醇的侧链酸进行酯化反应。由此形成的21种新紫杉烷类化合物在三种细胞系上进行了测试。它们的活性远低于紫杉醇。SIA衍生物的构效关系部分与紫杉醇一致,且大致可以辨别。

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