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ID: ALA2057195

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR.

Authors: Le PT, Cheng H, Ninkovic S, Plewe M, Huang X, Wang H, Bagrodia S, Sun S, Knighton DR, LaFleur Rogers CM, Pannifer A, Greasley S, Dalvie D, Zhang E.

Abstract: Lead optimization efforts that employed structure base drug design and physicochemical property based optimization leading to the discovery of a novel series of 4-methylpyrido pyrimidinone (MPP) are discussed. Synthesis and profile of 1, a PI3Kα/mTOR dual inhibitor, is highlighted.

CiteXplore: 22749419

DOI: 10.1016/j.bmcl.2012.05.100