Literature DB >> 21185177

Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.

Romain Noël1, Youseung Shin, Xinyi Song, Yuanjun He, Marcel Koenig, Weimin Chen, Yuan Yuan Ling, Li Lin, Claudia H Ruiz, Phil LoGrasso, Michael D Cameron, Derek R Duckett, Theodore M Kamenecka.   

Abstract

The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21185177      PMCID： PMC3081976          DOI： 10.1016/j.bmcl.2010.11.104

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


  35 in total

Review 1.  Mammalian mitogen-activated protein kinase signal transduction pathways activated by stress and inflammation.

Authors:  J M Kyriakis; J Avruch
Journal:  Physiol Rev       Date:  2001-04       Impact factor: 37.312

Review 2.  Regulation of MAP kinase signaling modules by scaffold proteins in mammals.

Authors:  Deborah K Morrison; Roger J Davis
Journal:  Annu Rev Cell Dev Biol       Date:  2003       Impact factor: 13.827

3.  SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase.

Authors:  B L Bennett; D T Sasaki; B W Murray; E C O'Leary; S T Sakata; W Xu; J C Leisten; A Motiwala; S Pierce; Y Satoh; S S Bhagwat; A M Manning; D W Anderson
Journal:  Proc Natl Acad Sci U S A       Date:  2001-11-20       Impact factor: 11.205

Review 4.  Targeting JNK3 for the treatment of neurodegenerative disorders.

Authors:  Lynn Resnick; Myles Fennell
Journal:  Drug Discov Today       Date:  2004-11-01       Impact factor: 7.851

5.  Joint damage and inflammation in c-Jun N-terminal kinase 2 knockout mice with passive murine collagen-induced arthritis.

Authors:  Zuoning Han; Lufen Chang; Yuji Yamanishi; Michael Karin; Gary S Firestein
Journal:  Arthritis Rheum       Date:  2002-03

6.  Nocodazole-induced p53-dependent c-Jun N-terminal kinase activation reduces apoptosis in human colon carcinoma HCT116 cells.

Authors:  Hong Zhang; Xiaoqing Shi; Qian-Jin Zhang; Maggie Hampong; Harry Paddon; Dewi Wahyuningsih; Steven Pelech
Journal:  J Biol Chem       Date:  2002-09-06       Impact factor: 5.157

7.  Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors.

Authors:  Ted Kamenecka; Rong Jiang; Xinyi Song; Derek Duckett; Weimin Chen; Yuan Yuan Ling; Jeff Habel; John D Laughlin; Jeremy Chambers; Mariana Figuera-Losada; Michael D Cameron; Li Lin; Claudia H Ruiz; Philip V LoGrasso
Journal:  J Med Chem       Date:  2010-01-14       Impact factor: 7.446

8.  A central role for JNK in obesity and insulin resistance.

Authors:  Jiro Hirosumi; Gürol Tuncman; Lufen Chang; Cem Z Görgün; K Teoman Uysal; Kazuhisa Maeda; Michael Karin; Gökhan S Hotamisligil
Journal:  Nature       Date:  2002-11-21       Impact factor: 49.962

Review 9.  Emerging treatments for asthma.

Authors:  Kate Blease; Alan Lewis; Heather K Raymon
Journal:  Expert Opin Emerg Drugs       Date:  2003-05       Impact factor: 4.191

Review 10.  JNK: a new therapeutic target for diabetes.

Authors:  Brydon L Bennett; Yoshitaka Satoh; Alan J Lewis
Journal:  Curr Opin Pharmacol       Date:  2003-08       Impact factor: 5.547
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  3 in total

1.  Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.

Authors:  Yuanjun He; Derek Duckett; Weimin Chen; Yuan Yuan Ling; Michael D Cameron; Li Lin; Claudia H Ruiz; Philip V Lograsso; Theodore M Kamenecka; Marcel Koenig
Journal:  Bioorg Med Chem Lett       Date:  2013-12-04       Impact factor: 2.823

Review 2.  Nuclear and cytosolic JNK signalling in neurons.

Authors:  Eleanor T Coffey
Journal:  Nat Rev Neurosci       Date:  2014-05       Impact factor: 34.870

3.  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
  3 in total

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