Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives

被引：21

作者：

Han, Fangbin ^{[1
]}

Lin, Songwen ^{[1
]}

Liu, Peng ^{[1
]}

Tao, Jing ^{[1
]}

Yi, Chongqin ^{[1
]}

Xu, Heng ^{[1
]}

机构：

[1] PKUCare Pharmaceut R&D Ctr, Biotech Innovat Works, Beijing 102206, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 18期

基金：

中国博士后科学基金;

关键词：

Phosphoinositide; 3-kinase; Mammalian target of rapamycin; Dual inhibitor; Anti-tumor activity; ANTITUMOR-ACTIVITY; HUMAN CANCER; CLASS-I; POTENT; DISCOVERY; TARGET; RAPAMYCIN; PI3K; PATHWAY; MTOR;

D O I：

10.1016/j.bmcl.2014.07.073

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway by PI3K/mTOR dual inhibitors provides a promising new approach to the treatment of cancers. In this Letter, we identified structurally novel and potent PI3K/ mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d] pyrimidine derivatives. Their synthesis and structure-activity relationships are reported. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：4538 / 4541

页数：4

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