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

…, M Plewe, X Huang, H Wang, S Bagrodia, S Sun…

文献索引：Le, Phuong T.; Cheng, Hengmiao; Ninkovic, Sacha; Plewe, Michael; Huang, Xiaojun; Wang, Hai; Bagrodia, Shubha; Sun, Shaoxian; Knighton, Daniel R.; Lafleur Rogers, Caroline M.; Pannifer, Andrew; Greasley, Samantha; Dalvie, Deepak; Zhang, Eric Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5098 - 5103

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被引用次数: 10

摘要

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.