Literature DB >> 16854050

Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.

Hongyu Zhao1, Michael D Serby, Zhili Xin, Bruce G Szczepankiewicz, Mei Liu, Christi Kosogof, Bo Liu, Lissa T J Nelson, Eric F Johnson, Sanyi Wang, Terry Pederson, Rebecca J Gum, Jill E Clampit, Deanna L Haasch, Cele Abad-Zapatero, Elizabeth H Fry, Cristina Rondinone, James M Trevillyan, Hing L Sham, Gang Liu.   

Abstract

C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK inhibitors could be valuable tools to study the therapeutic benefits of inhibiting these enzymes and as leads for potential drugs targeting JNKs. In this report, we disclose a series of potent and highly selective JNK inhibitors with good pharmacokinetic profiles.

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Year:  2006        PMID： 16854050     DOI： 10.1021/jm060465l

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  19 in total

1.  Lessons for fragment library design: analysis of output from multiple screening campaigns.

Authors:  I-Jen Chen; Roderick E Hubbard
Journal:  J Comput Aided Mol Des       Date:  2009-06-03       Impact factor: 3.686

2.  Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation.

Authors:  Ken-Ichi Kusakabe; Nobuyuki Ide; Yataro Daigo; Takeshi Itoh; Kenichi Higashino; Yousuke Okano; Genta Tadano; Yuki Tachibana; Yuji Sato; Makiko Inoue; Tooru Wada; Motofumi Iguchi; Takayuki Kanazawa; Yukichi Ishioka; Keiji Dohi; Sachie Tagashira; Yasuto Kido; Shingo Sakamoto; Kazuya Yasuo; Masahiro Maeda; Takahiko Yamamoto; Masayo Higaki; Takeshi Endoh; Kazuo Ueda; Takeshi Shiota; Hitoshi Murai; Yusuke Nakamura
Journal:  ACS Med Chem Lett       Date:  2012-06-06       Impact factor: 4.345

3.  Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.

Authors:  Yuanjun He; Theodore M Kamenecka; Youseung Shin; Xinyi Song; Rong Jiang; Romain Noel; Derek Duckett; Weimin Chen; Yuan Yuan Ling; Michael D Cameron; Li Lin; Susan Khan; Marcel Koenig; Philip V LoGrasso
Journal:  Bioorg Med Chem Lett       Date:  2011-01-22       Impact factor: 2.823

4.  Sampling Conformational Changes of Bound Ligands Using Nonequilibrium Candidate Monte Carlo and Molecular Dynamics.

Authors:  Sukanya Sasmal; Samuel C Gill; Nathan M Lim; David L Mobley
Journal:  J Chem Theory Comput       Date:  2020-02-24       Impact factor: 6.006

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.  Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors.

Authors:  Surya K De; Li-Hsing Chen; John L Stebbins; Thomas Machleidt; Megan Riel-Mehan; Russell Dahl; Vida Chen; Hongbin Yuan; Elisa Barile; Aras Emdadi; Ria Murphy; Maurizio Pellecchia
Journal:  Bioorg Med Chem       Date:  2009-02-26       Impact factor: 3.641

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.  Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.

Authors:  Surya K De; John L Stebbins; Li-Hsing Chen; Megan Riel-Mehan; Thomas Machleidt; Russell Dahl; Hongbin Yuan; Aras Emdadi; Elisa Barile; Vida Chen; Ria Murphy; Maurizio Pellecchia
Journal:  J Med Chem       Date:  2009-04-09       Impact factor: 7.446

9.  Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-Jun N-terminal kinase 3 (JNK3) over p38.

Authors:  Ted Kamenecka; Jeff Habel; Derek Duckett; Weimin Chen; Yuan Yuan Ling; Bozena Frackowiak; Rong Jiang; Youseung Shin; Xinyi Song; Philip LoGrasso
Journal:  J Biol Chem       Date:  2009-03-04       Impact factor: 5.157

10.  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
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