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Bioorg Med Chem Lett. 2009 Feb 1;19(3):766-9. doi: 10.1016/j.bmcl.2008.12.021. Epub 2008 Dec 10.

Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.

Author information

1
Wyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA.

Abstract

Thieno[2,3-b]pyridine-5-carbonitrile 16 with a 4-methyl-5-indolylamine at C-4 and a 5-methoxy-2-(dimethylamino)-methylphenyl group at C-2 had an IC(50) value of 16 nM for the inhibition of PKCtheta. While moderate inhibition of PKCdelta was also observed (IC(50)=130 nM), 16 had IC(50) values of greater than 5 microM against Lyn and other members of the Src kinase family.

PMID:
19111463
DOI:
10.1016/j.bmcl.2008.12.021
[Indexed for MEDLINE]

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