title: Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.
abstract: Starting from pyrazole HTS hit (1), a series of 1-aryl-1H-indazoles have been synthesized as JNK3 inhibitors with moderate selectivity against JNK1. SAR studies led to the synthesis of 5r as double digital nanomolar JNK3 inhibitor with good in vivo exposure.
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: Rong
authors.initials: R
authors.lastname: Jiang
authors.forename: Bozena
authors.initials: B
authors.lastname: Frackowiak
authors.forename: Youseung
authors.initials: Y
authors.lastname: Shin
authors.forename: Xinyi
authors.initials: X
authors.lastname: Song
authors.forename: Weimin
authors.initials: W
authors.lastname: Chen
authors.forename: Li
authors.initials: L
authors.lastname: Lin
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: D000814:Aniline Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D001921:Brain / Q000378:metabolism; D015195:Drug Design; D006207:Half-Life; D007191:Indazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D048057:Mitogen-Activated Protein Kinase 10 / Q000037:antagonists & inhibitors / Q000378:metabolism; D048055:Mitogen-Activated Protein Kinase 8 / Q000037:antagonists & inhibitors / Q000378:metabolism; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000814:Aniline Compounds; D007191:Indazoles; D047428:Protein Kinase Inhibitors; D048057:Mitogen-Activated Protein Kinase 10; D048031:JNK Mitogen-Activated Protein Kinases; D048055:Mitogen-Activated Protein Kinase 8