2. Academic Validation
  3. Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR

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

  • Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103. doi: 10.1016/j.bmcl.2012.05.100.
Phuong T Le 1,  Hengmiao Cheng,  Sacha Ninkovic,  Michael Plewe,  Xiaojun Huang,  Hai Wang,  Shubha Bagrodia,  Shaoxian Sun,  Daniel R Knighton,  Caroline M LaFleur Rogers,  Andrew Pannifer,  Samantha Greasley,  Deepak Dalvie,  Eric Zhang
Affiliations

Affiliation

  • 1 Cancer Chemistry, Pfizer Worldwide Research & Development, La Jolla Laboratories, Pfizer Inc., La Jolla, CA 92121, United States. [email protected]
PMID: 22749419 DOI: 10.1016/j.bmcl.2012.05.100
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.

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