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Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles |
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| Authors: | Boschelli Diane H Wu Biqi Barrios Sosa Ana Carolina Chen Joan Asselin Magda Cole Derek C Lee Julie Yang Xiaoke Chaudhary Divya |
| Institution: | aWyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA bWyeth Research, Inflammation, 200 Cambridge Park Drive, Cambridge, MA 02140, USA |
| Abstract: | The thieno2,3-b]pyridine-5-carbonitrile with a 5-indolylamine at C-4 and a phenyl group at C-2 had a moderate activity against PKCθ. Optimization of the groups at C-4 and C-2 led to analog 29, which has an IC50 value of 7.5 nM for the inhibition of PKCθ. |
| Keywords: | PKCθ Thieno[2 3-b]pyridine-5-carbonitrile |
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