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  • Title: Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.
    Author: Mortensen DS, Perrin-Ninkovic SM, Harris R, Lee BG, Shevlin G, Hickman M, Khambatta G, Bisonette RR, Fultz KE, Sankar S.
    Journal: Bioorg Med Chem Lett; 2011 Nov 15; 21(22):6793-9. PubMed ID: 21978683.
    Abstract:
    We report here the discovery of a novel series of selective mTOR kinase inhibitors. A series of imidazo[4,5-b]pyrazin-2-ones, represented by screening hit 1, was developed into lead compounds with excellent mTOR potency and exquisite kinase selectivity. Potent compounds from this series show >1000-fold selectivity over the related PI3Kα lipid kinase. Further, compounds such as 2 achieve mTOR pathway inhibition, blocking both mTORC1 and mTORC2 signaling, in PC3 cancer cells as measured by inhibition of pS6 and pAkt (S473).
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