Literature DB >> 19327989

Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.

Paul S Humphries1, Jennifer A Lafontaine, Charles S Agree, David Alexander, Ping Chen, Quyen-Quyen T Do, Lilian Y Li, Elizabeth A Lunney, Ranjan J Rajapakse, Karen Siegel, Sergei L Timofeevski, Tianlun Wang, David M Wilhite.   

Abstract

The development of a series of novel 4-substituted-2-aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, and the in vitro inhibitory value for a c-Jun cellular assay are discussed. Optimization of microsomal clearance led to the identification of 9c, whose kinase selectivity is reported.

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Year:  2009        PMID： 19327989     DOI： 10.1016/j.bmcl.2009.03.023

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


  6 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.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

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.  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

5.  Substituted aminopyrimidine protein kinase B (PknB) inhibitors show activity against Mycobacterium tuberculosis.

Authors:  Timothy M Chapman; Nathalie Bouloc; Roger S Buxton; Jasveen Chugh; Kathryn E A Lougheed; Simon A Osborne; Barbara Saxty; Stephen J Smerdon; Debra L Taylor; David Whalley
Journal:  Bioorg Med Chem Lett       Date:  2012-03-14       Impact factor: 2.823

6.  Structural basis and biological consequences for JNK2/3 isoform selective aminopyrazoles.

Authors:  HaJeung Park; Sarah Iqbal; Pamela Hernandez; Rudy Mora; Ke Zheng; Yangbo Feng; Philip LoGrasso
Journal:  Sci Rep       Date:  2015-01-27       Impact factor: 4.379
  6 in total

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