PI3K/mTOR双重抑制剂的研究进展  

Research progress on PI3K/mTOR dual inhibitors

作　　者：宣伟[1] 邵藤[1] 李义平[1] 张三奇[1] 

机构地区：[1]西安交通大学医学院药学系,陕西西安710061

出　　处：《现代药物与临床》2012年第2期133-137,共5页Drugs & Clinic

摘　　要：磷脂酰肌醇3-激酶/哺乳动物雷帕霉素靶蛋白(phosphoinosmde-3-kinase/the mammalian target of rapamycin,PI3K/mTOR)双重抑制剂已经成为抗肿瘤药物研发的热点之一。本文介绍芳基脲类和3-吡啶基杂环类等PI3K/mTOR双重抑制剂的化学结构,根据其结构特点及其与PI3Kγ共结晶模式,剖析了两类抑制剂药效团的基本结构。phosphoinosmde-3-kinase/the mammalian target of rapamycin（PI3K/mTOR） dual inhibitor is emerging as a hotspot in antitumor drugs research.This review introducesthe chemical structures of PI3K/mTOR dual inhibitors which can be sorted into arylureas and 3-pyridinyl heterocycles.The basic pharmacophore structures were suggested according to the structure characteristics of dual inhibitor and tits co-crystal structure with PI3K.

关 键 词：PI3K/mTOR双重抑制剂 药效团 抗肿瘤药物 

分 类 号：R979.1[医药卫生—药品]