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Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2011 Apr 15; Vol. 19 (8), pp. 2582-8. Date of Electronic Publication: 2011 Mar 12. - Publication Year :
- 2011
-
Abstract
- We report comprehensive structure-activity relationship studies on a novel series of c-Jun N-terminal kinase (JNK) inhibitors. Intriguingly, the compounds have a dual inhibitory activity by functioning as both ATP and JIP mimetics, possibly by binding to both the ATP binding site and to the docking site of the kinase. Several of such novel compounds display potent JNK inhibitory profiles both in vitro and in cell.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Adenosine Triphosphate
Binding Sites
Cell Line
Drug Design
Humans
Molecular Mimicry
Protein Binding
Protein Kinase Inhibitors pharmacology
Structure-Activity Relationship
Thiophenes chemistry
JNK Mitogen-Activated Protein Kinases antagonists & inhibitors
Protein Kinase Inhibitors chemical synthesis
Thiophenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 19
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 21458276
- Full Text :
- https://doi.org/10.1016/j.bmc.2011.03.017