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

The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with g...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-05, Vol.21 (9), p.2732-2735
Hauptverfasser:	Noël, Romain, Shin, Youseung, Song, Xinyi, He, Yuanjun, Koenig, Marcel, Chen, Weimin, Ling, Yuan Yuan, Lin, Li, Ruiz, Claudia H., LoGrasso, Phil, Cameron, Michael D., Duckett, Derek R., Kamenecka, Theodore M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Analytical, structural and metabolic biochemistry Biological and medical sciences c-Jun Enzyme Activation - drug effects enzyme inhibitors Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Inhibitory Concentration 50 JNK JNK Mitogen-Activated Protein Kinases - antagonists & inhibitors Kinase Medical sciences Miscellaneous mitogen-activated protein kinase Molecular Structure Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology pyridines pyrimidines Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Structure-Activity Relationship structure-activity relationships synthesis Transferases
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Zusammenfassung:	The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered. The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.11.104