Literature DB >> 16140012

Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.

Britt-Marie Swahn1, Fernando Huerta, Elisabet Kallin, Jonas Malmström, Tatjana Weigelt, Jenny Viklund, Patrick Womack, Yafeng Xue, Liselotte Ohberg.   

Abstract

The structure-based design and synthesis of a new series of c-Jun N-terminal kinase-3 inhibitors with selectivity against JNK1 and p38alpha is reported. The novel series of substituted 6-anilinoindazoles were designed based on a combination of hits from high throughput screening and X-ray crystal structure information of the compounds crystallized into the JNK3 ATP binding active site.

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Year:  2005        PMID： 16140012     DOI： 10.1016/j.bmcl.2005.06.083

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


  15 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.  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

3.  Suzuki-Miyaura cross-coupling of unprotected, nitrogen-rich heterocycles: substrate scope and mechanistic investigation.

Authors:  M Alexander Düfert; Kelvin L Billingsley; Stephen L Buchwald
Journal:  J Am Chem Soc       Date:  2013-08-16       Impact factor: 15.419

4.  Synthesis of 2,3-diarylsubstituted indazoles utilizing a Suzuki cross-coupling/deprotection/N-arylation sequence.

Authors:  James M Salovich; Craig W Lindsley; Corey R Hopkins
Journal:  Tetrahedron Lett       Date:  2010-07-21       Impact factor: 2.415

5.  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

6.  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

7.  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

8.  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

9.  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

10.  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
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