Combretastatin A-4顺式锁定衍生化研究进展

摘要/Abstract

摘要：

Combretastatin A-4（CA4）是天然抗肿瘤化合物，其顺式二苯乙烯构型对活性起关键作用。采用环状结构进行CA4的顺式构型锁定已成为目前结构改造的主要思路。本文从三元环、五元环、六元环锁定及骨架延伸锁定等方面综述了近年来CA4烯碳桥顺式锁定改造及衍生化的研究进展。

关键词: combretastatin A-4, 构效关系, 顺式锁定, 衍生化, 血管阻断剂

Abstract:

Combretastatin A-4 (CA4) is an important new generation vascular disrupting agent (VDA) from plant. The cis-stilbene configuration of which plays a crucial role on antitumor and anti-vascular activities. The ring formation in ethylene moiety has been considered to be the main idea for structure modification of CA4. The recent progress in cis-restricted derivations of CA4 representing by three, five, six-membered ring formation as well as skeleton extension has been reviewed.

Key words: combretastatin A-4, SAR, cis-restriction, derivation, VDA

肖春芬，孙洪宜，魏文，都建立，邹永. Combretastatin A-4顺式锁定衍生化研究进展[J]. 天然产物研究与开发, 2011, 23(1): 169-185.

XIAO Chun-Fen, SUN Hong-Yi, WEI Wen, DU Jian-Li, ZOU Yong. Progress in cis-Restricted Derivations of Combretastatin A-4[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2011, 23(1): 169-185.

参考文献

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