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

ABSTRACT: 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.

SUBMITTER: Yang C

PROVIDER: S-EPMC5554905 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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

Yang Chengbin C Zhang Xi X Wang Yi Y Yang Yongtai Y Liu Xiaofeng X Deng Mingli M Jia Yu Y Ling Yun Y Meng Ling-Hua LH Zhou Yaming Y

ACS medicinal chemistry letters 20170726 8

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 prolif ...[more]

PMID: 28835805

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