title: Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors.
abstract: A new series of 2-thioether-benzothiazoles has been synthesized and evaluated for JNK inhibition. The SAR studies led to the discovery of potent, allosteric JNK inhibitors with selectivity against p38.
authors.affiliation: Burnham Institute for Medical Research, La Jolla, CA 92037, USA.
authors.forename: Surya K
authors.initials: SK
authors.lastname: De
authors.forename: Li-Hsing
authors.initials: LH
authors.lastname: Chen
authors.forename: John L
authors.initials: JL
authors.lastname: Stebbins
authors.forename: Thomas
authors.initials: T
authors.lastname: Machleidt
authors.forename: Megan
authors.initials: M
authors.lastname: Riel-Mehan
authors.forename: Russell
authors.initials: R
authors.lastname: Dahl
authors.forename: Vida
authors.initials: V
authors.lastname: Chen
authors.forename: Hongbin
authors.initials: H
authors.lastname: Yuan
authors.forename: Elisa
authors.initials: E
authors.lastname: Barile
authors.forename: Aras
authors.initials: A
authors.lastname: Emdadi
authors.forename: Ria
authors.initials: R
authors.lastname: Murphy
authors.forename: Maurizio
authors.initials: M
authors.lastname: Pellecchia
mesh_terms: D048868:Adaptor Proteins, Signal Transducing / Q000378:metabolism; D000494:Allosteric Regulation; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D003198:Computer Simulation; D055808:Drug Discovery; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010446:Peptide Fragments / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D048868:Adaptor Proteins, Signal Transducing; D052160:Benzothiazoles; C520352:JNK-interacting protein 1 (153-163); D010446:Peptide Fragments; D047428:Protein Kinase Inhibitors; D048031:JNK Mitogen-Activated Protein Kinases; D048051:p38 Mitogen-Activated Protein Kinases