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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Adaptor Proteins, Signal Transducing / metabolism
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Allosteric Regulation
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Benzothiazoles / chemical synthesis
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Benzothiazoles / chemistry*
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Benzothiazoles / pharmacology
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Computer Simulation
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Drug Discovery
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JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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JNK Mitogen-Activated Protein Kinases / metabolism
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Peptide Fragments / metabolism
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacology
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors
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p38 Mitogen-Activated Protein Kinases / metabolism
Substances
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Adaptor Proteins, Signal Transducing
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Benzothiazoles
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JNK-interacting protein 1 (153-163)
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Peptide Fragments
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Protein Kinase Inhibitors
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JNK Mitogen-Activated Protein Kinases
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p38 Mitogen-Activated Protein Kinases