title: Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.
abstract: 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.
authors.affiliation: Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6098, USA. mei.liu@abbott.com
authors.forename: Mei
authors.initials: M
authors.lastname: Liu
authors.forename: Sanyi
authors.initials: S
authors.lastname: Wang
authors.forename: Jill E
authors.initials: JE
authors.lastname: Clampit
authors.forename: Rebecca J
authors.initials: RJ
authors.lastname: Gum
authors.forename: Deanna L
authors.initials: DL
authors.lastname: Haasch
authors.forename: Cristina M
authors.initials: CM
authors.lastname: Rondinone
authors.forename: James M
authors.initials: JM
authors.lastname: Trevillyan
authors.forename: Cele
authors.initials: C
authors.lastname: Abad-Zapatero
authors.forename: Elizabeth H
authors.initials: EH
authors.lastname: Fry
authors.forename: Hing L
authors.initials: HL
authors.lastname: Sham
authors.forename: Gang
authors.initials: G
authors.lastname: Liu
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D008968:Molecular Conformation; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000814:Aniline Compounds; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D011743:Pyrimidines; D048031:JNK Mitogen-Activated Protein Kinases