Literature DB >> 17459703

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

Mahbub Alam1, Rebekah E Beevers, Tom Ceska, Richard J Davenport, Karen M Dickson, Mara Fortunato, Lewis Gowers, Alan F Haughan, Lynwen A James, Mark W Jones, Natasha Kinsella, Christopher Lowe, Johannes W G Meissner, Anne-Lise Nicolas, Benjamin G Perry, David J Phillips, William R Pitt, Adam Platt, Andrew J Ratcliffe, Andrew Sharpe, Laura J Tait.   

Abstract

The development of a series of novel aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, JNK2 and CDK2, and the in vitro inhibitory value for a c-Jun cellular assay are discussed.

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Year:  2007        PMID： 17459703     DOI： 10.1016/j.bmcl.2007.03.078

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


  11 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.  Improved Description of Sulfur Charge Anisotropy in OPLS Force Fields: Model Development and Parameterization.

Authors:  Xin Cindy Yan; Michael J Robertson; Julian Tirado-Rives; William L Jorgensen
Journal:  J Phys Chem B       Date:  2017-06-29       Impact factor: 2.991

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.  Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.

Authors:  Ke Zheng; Chul Min Park; Sarah Iqbal; Pamela Hernandez; HaJeung Park; Philip V LoGrasso; Yangbo Feng
Journal:  ACS Med Chem Lett       Date:  2015-03-02       Impact factor: 4.345

5.  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

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.  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

8.  Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.

Authors:  Wenjun Zhou; Dalia Ercan; Liang Chen; Cai-Hong Yun; Danan Li; Marzia Capelletti; Alexis B Cortot; Lucian Chirieac; Roxana E Iacob; Robert Padera; John R Engen; Kwok-Kin Wong; Michael J Eck; Nathanael S Gray; Pasi A Jänne
Journal:  Nature       Date:  2009-12-24       Impact factor: 49.962

9.  Discovery of potent and selective covalent inhibitors of JNK.

Authors:  Tinghu Zhang; Francisco Inesta-Vaquera; Mario Niepel; Jianming Zhang; Scott B Ficarro; Thomas Machleidt; Ting Xie; Jarrod A Marto; NamDoo Kim; Taebo Sim; John D Laughlin; Hajeung Park; Philip V LoGrasso; Matt Patricelli; Tyzoon K Nomanbhoy; Peter K Sorger; Dario R Alessi; Nathanael S Gray
Journal:  Chem Biol       Date:  2012-01-27

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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