Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 5, Pages 1486-1492Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.12.047
Keywords
c-Jun N-terminal kinase (JNK); CDK; Kinase inhibitor; Kinase selectivity
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A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and selective JNK inhibitor, compound 24f (JNK1 and 2 IC50 = 16 and 66 nM, respectively), with bioavailability in rats and suitable for further in vivo pharmacological evaluation. (c) 2013 Elsevier Ltd. All rights reserved.
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