Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies

A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selectivity profile and the crystal structure of 2b are a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (3), p.668-672
Hauptverfasser:	Liu, Mei, Wang, Sanyi, Clampit, Jill E., Gum, Rebecca J., Haasch, Deanna L., Rondinone, Cristina M., Trevillyan, James M., Abad-Zapatero, Cele, Fry, Elizabeth H., Sham, Hing L., Liu, Gang
Format:	Artikel
Sprache:	eng
Schlagworte:	Aniline Compounds - chemical synthesis Aniline Compounds - pharmacology Biological and medical sciences Crystallography, X-Ray Diabetes Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General and cellular metabolism. Vitamins Indicators and Reagents JNK inhibitors JNK Mitogen-Activated Protein Kinases - antagonists & inhibitors Kinase Magnetic Resonance Spectroscopy Medical sciences Models, Molecular Molecular Conformation Obesity Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - pharmacology Structure-Activity Relationship
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Zusammenfassung:	A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selectivity profile and the crystal structure of 2b are also described. A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selectivity profile and the crystal structure of 2b are also described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.10.093