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ID: ALA4190336

Journal: ACS Med Chem Lett

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

Authors: Yang C, Zhang X, Wang Y, Yang Y, Liu X, Deng M, Jia Y, Ling Y, Meng LH, Zhou Y.

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.

CiteXplore: 28835805

DOI: 10.1021/acsmedchemlett.7b00222