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

Abstract 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.