Literature DB >> 19433357

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

Youseung Shin1, Weiming Chen, Jeff Habel, Derek Duckett, Yuan Yuan Ling, Marcel Koenig, Yuanjun He, Tomas Vojkovsky, Philip LoGrasso, Theodore M Kamenecka.   

Abstract

A novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from a high-throughput-screening hit. Through the optimization of the piperazine amide 1, several potent compounds were discovered. The X-ray crystal structure of 4g showed a unique binding mode different from other well known JNK3 inhibitors.

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Year:  2009        PMID： 19433357      PMCID： PMC2737472          DOI： 10.1016/j.bmcl.2009.03.086

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


  27 in total

Review 1.  The c-Jun N-terminal protein kinase family of mitogen-activated protein kinases (JNK MAPKs).

Authors:  R K Barr; M A Bogoyevitch
Journal:  Int J Biochem Cell Biol       Date:  2001-11       Impact factor: 5.085

Review 2.  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

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.  Inhibitors of the tyrosine kinase signaling cascade for asthma.

Authors:  W S Fred Wong
Journal:  Curr Opin Pharmacol       Date:  2005-06       Impact factor: 5.547

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.  A critical role of neural-specific JNK3 for ischemic apoptosis.

Authors:  Chia-Yi Kuan; Alan J Whitmarsh; Derek D Yang; Guanghong Liao; Aryn J Schloemer; Chen Dong; Jue Bao; Kenneth J Banasiak; Gabriel G Haddad; Richard A Flavell; Roger J Davis; Pasko Rakic
Journal:  Proc Natl Acad Sci U S A       Date:  2003-12-01       Impact factor: 11.205

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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  9 in total

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

Authors:  Romain Noël; 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
Journal:  Bioorg Med Chem Lett       Date:  2010-12-01       Impact factor: 2.823

2.  Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors.

Authors:  Igor A Schepetkin; Liliya N Kirpotina; Andrei I Khlebnikov; Tracey S Hanks; Irina Kochetkova; David W Pascual; Mark A Jutila; Mark T Quinn
Journal:  Mol Pharmacol       Date:  2012-03-20       Impact factor: 4.436

3.  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

4.  Small Molecule c-jun-N-terminal Kinase (JNK) Inhibitors Protect Dopaminergic Neurons in a Model of Parkinson's Disease.

Authors:  Jeremy W Chambers; Alok Pachori; Shannon Howard; Michelle Ganno; Donald Hansen; Ted Kamenecka; Xinyi Song; Derek Duckett; Weimin Chen; Yuan Yuan Ling; Lisa Cherry; Michael D Cameron; Li Lin; Claudia H Ruiz; Philip Lograsso
Journal:  ACS Chem Neurosci       Date:  2011-04-20       Impact factor: 4.418

5.  Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.

Authors:  Surya K De; Elisa Barile; Vida Chen; John L Stebbins; Jason F Cellitti; Thomas Machleidt; Coby B Carlson; Li Yang; Russell Dahl; Maurizio Pellecchia
Journal:  Bioorg Med Chem       Date:  2011-03-12       Impact factor: 3.641

6.  N-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors.

Authors:  Yangbo Feng; HaJeung Park; Jae Cheon Ryu; Sung Ok Yoon
Journal:  ACS Med Chem Lett       Date:  2021-09-21       Impact factor: 4.632

7.  Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.

Authors:  Surya K De; Vida Chen; John L Stebbins; Li-Hsing Chen; Jason F Cellitti; Thomas Machleidt; Elisa Barile; Megan Riel-Mehan; Russell Dahl; Li Yang; Aras Emdadi; Ria Murphy; Maurizio Pellecchia
Journal:  Bioorg Med Chem       Date:  2009-12-11       Impact factor: 3.641

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.  In Vitro and In Silico Study to Assess Toxic Mechanisms of Hybrid Molecules of Quinone-Benzocaine as Plastoquinone Analogues in Breast Cancer Cells.

Authors:  Ayse Mine Yilmaz Goler; Ayse Tarbin Jannuzzi; Nilüfer Bayrak; Mahmut Yıldız; Hatice Yıldırım; Masami Otsuka; Mikako Fujita; Mohamed O Radwan; Amaç Fatih TuYuN
Journal:  ACS Omega       Date:  2022-08-15
  9 in total

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