低毒性PI3K/mTOR抑制剂的研究进展  

Research progress on PI3K/mTOR dual inhibitors with low toxicity

作　　者：王晓朦[1] 辛敏行[1] 张三奇[1] 

机构地区：[1]西安交通大学药学院,陕西西安710061

出　　处：《中国药物化学杂志》2016年第3期217-224,270,共9页Chinese Journal of Medicinal Chemistry

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.

关 键 词：PI3K/m TOR抑制剂 抗肿瘤 毒性 

分 类 号：R979.1[医药卫生—药品]