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低毒性PI3K/mTOR抑制剂的研究进展

Research progress on PI3K/mTOR dual inhibitors with low toxicity
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摘要 近年来,已有多种PI3K/mTOR双重抑制剂进入抗肿瘤临床试验,但是这些双重抑制剂的临床有效性不足,且显示出一定的毒性。本文简要介绍了PI3K/mTOR双重抑制剂的结构、毒性及通过结构优化发现的低毒性PI3K/mTOR双重抑制剂。 Phosphoinositide-3-kinase/the mammalian target of rapamycin（PI3K/mT0R） dual inhibitors have been developed into clinic trial to treat cancer.The emerging clinical data show limited single agent activity of the inhibitors targeting PI3 K and/or mTOR at tolerated doses.This review introduces the new discovery on the chemical structures and toxicity of PI3K/mT0 R dual inhibitors,summarizes the new discovery,made in our research group pn structural optimization to reduce toxicity of PI3K/mT0 R inhibitors.
作者 王晓朦 辛敏行 张三奇
机构地区 西安交通大学药学院
出处 《中国药物化学杂志》 CAS CSCD 2016年第3期217-224,270,共9页 Chinese Journal of Medicinal Chemistry
关键词 PI3K/m TOR抑制剂 抗肿瘤 毒性 PI3K/mT0R dual inhibitor antitumor drug toxicity
分类号 R979.1 [医药卫生—药品]
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参考文献44

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中国药物化学杂志
2016年 第3期

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