Title : Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Pub. Date : 2010 Mar 15

PMID : 20153643






1 Functional Relationships(s)
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1 Analog 8, a 3-pyridinecarbonitrile with an (E)-2-[6-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]vinyl group at C-5, had an IC(50) value of 1.1 nM for the inhibition of PKCtheta and potently blocked the production of IL-2 in both stimulated murine T cells (IC(50)=34 nM) and human whole blood (IC(50)=500 nM). 3-cyanopyridine interleukin 2 Mus musculus