Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors.
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.
De
Surya K
SK
Burnham Institute for Medical Research, La Jolla, CA 92037, USA.
Chen
Li-Hsing
LH
Stebbins
John L
JL
Machleidt
Thomas
T
Riel-Mehan
Megan
M
Dahl
Russell
R
Chen
Vida
V
Yuan
Hongbin
H
Barile
Elisa
E
Emdadi
Aras
A
Murphy
Ria
R
Pellecchia
Maurizio
M
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
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