title: Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
abstract: The structure-activity relationships of 5,6-positions of aminopyridine carboxamide-based c-Jun N-terminal Kinase (JNK) inhibitors were explored to expand interaction with the kinase specificity and ribose-binding pockets. The syntheses of analogues and the impact of structural modification on in vitro potency and cellular activity are described.
authors.affiliation: Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. gang.liu@abbott.com
authors.forename: Gang
authors.initials: G
authors.lastname: Liu
authors.forename: Hongyu
authors.initials: H
authors.lastname: Zhao
authors.forename: Bo
authors.initials: B
authors.lastname: Liu
authors.forename: Zhili
authors.initials: Z
authors.lastname: Xin
authors.forename: Mei
authors.initials: M
authors.lastname: Liu
authors.forename: Christi
authors.initials: C
authors.lastname: Kosogof
authors.forename: Bruce G
authors.initials: BG
authors.lastname: Szczepankiewicz
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: James M
authors.initials: JM
authors.lastname: Trevillyan
authors.forename: Hing L
authors.initials: HL
authors.lastname: Sham
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D000631:Aminopyridines / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D011485:Protein Binding; D012266:Ribose / Q000378:metabolism; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000577:Amides; D000631:Aminopyridines; D004791:Enzyme Inhibitors; D012266:Ribose; D048031:JNK Mitogen-Activated Protein Kinases