Literature DB >> 18606543

2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.

L Nathan Tumey1, Diane H Boschelli, Julie Lee, Divya Chaudhary.   

Abstract

A series of 2-alkenyl thieno[2,3-b]pyridine inhibitors of PKCtheta were synthesized as potential inflammatory modulators. This series led to the discovery of 2-alkenyl amides, which are exceptionally potent and selective inhibitors of PKCtheta. Compound 8 has an IC(50) of 3.8nM against PKCtheta and shows excellent selectivity over a variety of PKC isoforms.

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Year:  2008        PMID: 18606543     DOI: 10.1016/j.bmcl.2008.06.040

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


  6 in total

1.  Synthesis of multicyclic pyridine and quinoline derivatives via intramolecular C-H bond functionalization.

Authors:  Sirilata Yotphan; Robert G Bergman; Jonathan A Ellman
Journal:  Org Lett       Date:  2010-07-02       Impact factor: 6.005

2.  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 3.  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

4.  Bis(2-amino-5-benzyl-3-eth-oxy-carbonyl-4,5,6,7-tetra-hydro-thieno[3,2-c]pyridin-5-ium) bis-(4-meth-oxy-phen-yl)di-phos-phon-ate.

Authors:  Mehmet Akkurt; Joel T Mague; Shaaban K Mohamed; Sabry H H Younes; Mustafa R Albayati
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-02-22

5.  Crystal structure of (4-meth-oxy-phen-yl)[(4-meth-oxy-phen-yl)phospho-nato]dioxidophosphate(1-) 2-amino-6-benzyl-3-eth-oxy-carbon-yl-4,5,6,7-tetra-hydro-thieno[2,3-c]pyridin-6-ium.

Authors:  Joel T Mague; Shaaban K Mohamed; Mehmet Akkurt; Sabry H H Younes; Essam K Ahmed; Mustafa R Albayati
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-11-28

6.  3-Cyanoallyl boronates are versatile building blocks in the synthesis of polysubstituted thiophenes.

Authors:  Wenjie Shao; Sherif J Kaldas; Andrei K Yudin
Journal:  Chem Sci       Date:  2017-04-18       Impact factor: 9.825

  6 in total

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