Literature DB >> 19111463

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

Biqi Wu1, Diane H Boschelli, Julie Lee, Xiaoke Yang, Divya Chaudhary.   

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.

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Year:  2008        PMID: 19111463     DOI: 10.1016/j.bmcl.2008.12.021

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Prediction of PKCθ inhibitory activity using the Random Forest Algorithm.

Authors:  Ming Hao; Yan Li; Yonghua Wang; Shuwei Zhang
Journal:  Int J Mol Sci       Date:  2010-09-20       Impact factor: 5.923

Review 2.  The Novel PKCθ from Benchtop to Clinic.

Authors:  Rouba Hage-Sleiman; Asmaa B Hamze; Lina Reslan; Hadile Kobeissy; Ghassan Dbaibo
Journal:  J Immunol Res       Date:  2015-05-19       Impact factor: 4.818

  2 in total

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