Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 13, Pages 5323-5333Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b00626
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- Celgene San Diego CLMD group
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We report here the synthesis and structure-activity relationship (SAR) of a novel series of mammalian target of rapamycin (mTOR) kinase inhibitors. A series of 4,6- or 1,7-disubstituted-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-ones were optimized for in vivo efficacy. These efforts resulted in the identification of compounds with excellent mTOR kinase inhibitory potency, with exquisite kinase selectivity over the related lipid kinase PI3K. The improved PK properties of this series allowed for exploration of in vivo efficacy and ultimately the selection of CC-223 for clinical development.
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