Optimization of 5-phenyl-3-pyridinecarbonitriles as PKC theta inhibitors

[摘要]：The key intermediate, 4-chloro-5-iodo-3-pyridinecarbonitrile, allowed for ready optimization of the PKC theta inhibitory activity of a series of 3-pyridinecarbonitriles. Analog 13b with a 4-methylindol-5-ylamino group at C-4 and a 4-(2-(4-methylpiperazin-1-yl)ethoxy) phenyl group at C-5 had an IC50 value of 7.4 nM for the inhibition of PKC theta. (C) 2009 Elsevier Ltd. All rights reserved.

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