磷脂酰肌醇3-激酶/哺乳動物雷帕霉素靶蛋白（phosphoinosmde-3-kinase/the mammalian target of rapamycin，PI3K/mTOR）雙重抑制劑已經(jīng)成為抗腫瘤藥物研發(fā)的熱點之一。本文介紹芳基脲類和3-吡啶基雜環(huán)類等PI3K/mTOR雙重抑制劑的化學(xué)結(jié)構(gòu)，根據(jù)其結(jié)構(gòu)特點及其與PI3Kγ共結(jié)晶模式，剖析了兩類抑制劑藥效團的基本結(jié)構(gòu)。

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.