Literature DB >> 17107797

Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.

Mei Liu1, Sanyi Wang, Jill E Clampit, Rebecca J Gum, Deanna L Haasch, Cristina M Rondinone, James M Trevillyan, Cele Abad-Zapatero, Elizabeth H Fry, Hing L Sham, Gang Liu.   

Abstract

A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selectivity profile and the crystal structure of 2b are also described.

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Year:  2006        PMID： 17107797     DOI： 10.1016/j.bmcl.2006.10.093

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


  13 in total

1.  Exploring conformational search protocols for ligand-based virtual screening and 3-D QSAR modeling.

Authors:  Daniel Cappel; Steven L Dixon; Woody Sherman; Jianxin Duan
Journal:  J Comput Aided Mol Des       Date:  2014-11-19       Impact factor: 3.686

2.  Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

Authors:  Matthew P Martin; Yunting Luo; Roberta Pireddu; Hua Yang; Harsukh Gevariya; Harshani R Lawrence; Sevil Ozcan; Jin-Yi Zhu; Robert Kendig; Mercedes Rodriguez; Roy Elias; Jin Q Cheng; Saïd M Sebti; Ernst Schonbrunn; Nicholas J Lawrence
Journal:  J Med Chem       Date:  2012-08-30       Impact factor: 7.446

3.  Posttranslational modification of vesicular stomatitis virus glycoprotein, but not JNK inhibition, is the antiviral mechanism of SP600125.

Authors:  Sabrina Marozin; Jennifer Altomonte; Sibylle Apfel; Phat X Dinh; Enrico N De Toni; Antonia Rizzani; Andreas Nüssler; Nobuyuki Kato; Roland M Schmid; Asit K Pattnaik; Oliver Ebert
Journal:  J Virol       Date:  2012-02-15       Impact factor: 5.103

4.  Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.

Authors:  Ke Zheng; Chul Min Park; Sarah Iqbal; Pamela Hernandez; HaJeung Park; Philip V LoGrasso; Yangbo Feng
Journal:  ACS Med Chem Lett       Date:  2015-03-02       Impact factor: 4.345

5.  Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors.

Authors:  Youseung Shin; Weiming Chen; Jeff Habel; Derek Duckett; Yuan Yuan Ling; Marcel Koenig; Yuanjun He; Tomas Vojkovsky; Philip LoGrasso; Theodore M Kamenecka
Journal:  Bioorg Med Chem Lett       Date:  2009-03-26       Impact factor: 2.823

6.  Analysis of conditions affecting auto-phosphorylation of human kinases during expression in bacteria.

Authors:  Amit Shrestha; Garth Hamilton; Eric O'Neill; Stefan Knapp; Jonathan M Elkins
Journal:  Protein Expr Purif       Date:  2011-10-01       Impact factor: 1.650

7.  2D QSAR Studies of Several Potent Aminopyridine, Anilinopyrimidine and Pyridine Carboxamide-based JNK Inhibitors.

Authors:  S Sharma; B Bagchi; S Mukhopadhyay; A K Bothra
Journal:  Indian J Pharm Sci       Date:  2011-03       Impact factor: 0.975

8.  Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.

Authors:  Ke Zheng; Sarah Iqbal; Pamela Hernandez; HaJeung Park; Philip V LoGrasso; Yangbo Feng
Journal:  J Med Chem       Date:  2014-11-21       Impact factor: 7.446

9.  Anthrapyrazolone analogues intercept inflammatory JNK signals to moderate endotoxin induced septic shock.

Authors:  Karothu Durga Prasad; Jamma Trinath; Ansuman Biswas; Kanagaraj Sekar; Kithiganahalli N Balaji; Tayur N Guru Row
Journal:  Sci Rep       Date:  2014-11-27       Impact factor: 4.379

10.  Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.

Authors:  Daren Fearon; Isaac M Westwood; Rob L M van Montfort; Richard Bayliss; Keith Jones; Vassilios Bavetsias
Journal:  Bioorg Med Chem       Date:  2018-04-17       Impact factor: 3.641
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