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Synthesis and PKCθ inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles

The synthesis and PKCθ inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles is described. SAR studies led to the identification of compound 12d as a potent inhibitor of PKCθ. A series of 4-indolylamino-5-phenyl-3-pyridinecarbonitrile inhibitors of PKCθ were synthesized...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-05, Vol.19 (9), p.2461-2463
Main Authors: Dushin, Russell G., Nittoli, Thomas, Ingalls, Charles, Boschelli, Diane H., Cole, Derek C., Wissner, Allan, Lee, Julie, Yang, Xiaoke, Morgan, Paul, Brennan, Agnes, Chaudhary, Divya
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Language:English
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Summary:The synthesis and PKCθ inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles is described. SAR studies led to the identification of compound 12d as a potent inhibitor of PKCθ. A series of 4-indolylamino-5-phenyl-3-pyridinecarbonitrile inhibitors of PKCθ were synthesized as potential anti-inflammatory agents. The effects of specific substitution on the 5-phenyl moiety and variations of the positional isomers of the 4-indolylamino substituent were explored. This study led to the discovery of compound 12d, which had an IC 50 value of 18 nM for the inhibition of PKCθ.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.03.053