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C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCθ inhibitors: Part II
Amar S. Prashad ,
Daniel Wang ,
Joan Subrath ,
Biqi Wu ,
Melissa Lin ,
Mei-Yi Zhang ,
Natasha Kagan ,
Julie Lee ,
Xiaoke Yang ,
Agnes Brennan ,
Divya Chaudhary ,
Xin Xu ,
Louis Leung ,
Jack Wang ,
Diane H. Boschelli
October 2009
October 2009
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Abstract
We previously reported that a 3-pyridinecarbonitrile analog with a furan substituent
at C-5 and a 4-methylindol-5-ylamino substituent at C-4, 1, was a potent inhibitor
of PKCtheta (IC50=4.5 nM). Replacement of the C-5 furan ring of 1 with bicyclic heteroaryl
rings, led to compounds with significantly improved potency against PKCtheta. Analog
6b with a 4-methylindol-5-ylamino group at C-4 and a 5-[(4-methylpiperazin-1-yl)methyl]-1-benzofuran-2-yl
group at C-5 had an IC50 value of 0.28 nM for the inhibition of PKCtheta.