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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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Published in: | Bioorganic & medicinal chemistry letters 2009-05, Vol.19 (9), p.2461-2463 |
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Main Authors: | , , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2009.03.053 |