大环骨架在抗肿瘤药物研究开发中的应用  

Macrocycles in Oncology Drug Discovery

作　　者：胡亮[1] 周明[1] 刘瑞环[1] 余聂芳[1] 

机构地区：[1]中南大学药学院分子设计与药物发现研究所,湖南长沙410013

出　　处：《广州化工》2013年第9期3-4,12,共3页GuangZhou Chemical Industry

基　　金：国家自然科学基金项目(30873137;81172927)

摘　　要：大环结构修饰位点多,并且本身具有多样性与新颖性。这些特点使得大环结构作为母核或者基本结构单元,正在药物研究开发中得到越来越广泛的应用。本文就近几年抗肿瘤药物研究开发中合成类大环化合物骨架的构建和修饰对靶点亲和力,靶点选择性及自身理化性质的影响作一综述。The macrocyclic skeletons were emerging as important templates for medicinal chemists in the field of drug discovery, owning to their diverse modification points and their novelty. The effects of macrocyclization on potency, selectivity and physicochemical properties were mainly discussed, concentrating on recent case histories in oncology drug discovery.

关 键 词：大环骨架 结构修饰 抗肿瘤 新药开发 

分 类 号：R9[医药卫生—药学]