Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity

被引：27

作者：

Yang, Chengbin ^{[1
]}

Zhang, Xi ^{[2
]}

Wang, Yi ^{[2
]}

Yang, Yongtai ^{[1
]}

Liu, Xiaofeng ^{[1
]}

Deng, Mingli ^{[1
]}

Jia, Yu ^{[1
]}

Ling, Yun ^{[1
]}

Meng, Ling-hua ^{[2
]}

Zhou, Yaming ^{[1
]}

机构：

[1] Fudan Univ, Shanghai Key Lab Mol Catalysis & Innovat Mat, Dept Chem, Shanghai 200433, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2017年 / 8卷 / 08期

关键词：

PI3K; PI3K/mTOR; oncology; 1H-pyrrolo[2,3-b] pyridine; cancer therapy; PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS; (PI3K)/MAMMALIAN TARGET; PI3K/AKT/MTOR PATHWAY; ANTITUMOR-ACTIVITY; KINASE INHIBITOR; CANCER-THERAPY; HIGHLY POTENT; RAPAMYCIN; IDENTIFICATION; DESIGN;

D O I：

10.1021/acsmedchemlett.7b00222

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/AKT/mTOR, which provides a promising new approach for the molecularly targeted cancer therapy. In this work, a novel series of 7-azaindole scaffold derivatives was discovered by the fragment-based growing strategy. The structure-activity relationship profiles identified that the 7-azaindole scaffold derivatives exhibit potent activity against PI3K at molecular and cellular levels as well as cell proliferation in a panel of human tumor cells.

引用

页码：875 / 880

页数：6

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