Structural highlights
Publication Abstract from PubMed
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 PI3Kalpha/mTOR dual inhibitor, is highlighted.
Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kalpha and mTOR.,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 Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103. doi:, 10.1016/j.bmcl.2012.05.100. Epub 2012 Jun 6. PMID:22749419[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ 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. Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kalpha and mTOR. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103. doi:, 10.1016/j.bmcl.2012.05.100. Epub 2012 Jun 6. PMID:22749419 doi:http://dx.doi.org/10.1016/j.bmcl.2012.05.100