title: Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.
abstract: 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.
authors.affiliation: Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
authors.forename: Romain
authors.initials: R
authors.lastname: Noël
authors.forename: Youseung
authors.initials: Y
authors.lastname: Shin
authors.forename: Xinyi
authors.initials: X
authors.lastname: Song
authors.forename: Yuanjun
authors.initials: Y
authors.lastname: He
authors.forename: Marcel
authors.initials: M
authors.lastname: Koenig
authors.forename: Weimin
authors.initials: W
authors.lastname: Chen
authors.forename: Yuan Yuan
authors.initials: YY
authors.lastname: Ling
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.forename: Claudia H
authors.initials: CH
authors.lastname: Ruiz
authors.forename: Phil
authors.initials: P
authors.lastname: LoGrasso
authors.forename: Michael D
authors.initials: MD
authors.lastname: Cameron
authors.forename: Derek R
authors.initials: DR
authors.lastname: Duckett
authors.forename: Theodore M
authors.initials: TM
authors.lastname: Kamenecka
mesh_terms: D004789:Enzyme Activation / Q000187:drug effects; D020128:Inhibitory Concentration 50; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011743:Pyrimidines; C031280:pyrazole; D048031:JNK Mitogen-Activated Protein Kinases