| PI3K/mTOR双重抑制剂的研究进展 |
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| 引用本文： | 宣 伟,邵 藤,李义平,张三奇.PI3K/mTOR双重抑制剂的研究进展[J].现代药物与临床,2012,27(2):133-137. |
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| 作者姓名： | 宣 伟 邵 藤 李义平 张三奇 |
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| 作者单位： | 西安交通大学医学院药学系 |
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| 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。
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| 关 键 词： | PI3K/mTOR双重抑制剂 药效团 抗肿瘤药物 |
Research progress on PI3K/mTOR dual inhibitors |
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| XUAN Wei,SHAO Teng,LI Yi-ping and ZHANG San-qi.Research progress on PI3K/mTOR dual inhibitors[J].Drugs & Clinic,2012,27(2):133-137. |
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| Authors: | XUAN Wei SHAO Teng LI Yi-ping and ZHANG San-qi |
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| Institution: | Department of Pharmacy,School of Medicine,Xi’an Jiaotong University,Xi’an 710061,China |
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| Abstract: | 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. |
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| Keywords: | phosphoinosmde-3-kinase/the mammalian target of rapamycin(PI3K/mTOR) dual inhibitor pharmacophore antitumor drugs |
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