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.