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Bioorg Med Chem. 2011 Apr 15;19(8):2582-8. doi: 10.1016/j.bmc.2011.03.017. Epub 2011 Mar 12.

Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.

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1
Sanford-Burnham Medical Research Institute, La Jolla, CA 92037, USA.

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.

PMID:
21458276
PMCID:
PMC3089059
DOI:
10.1016/j.bmc.2011.03.017
[Indexed for MEDLINE]
Free PMC Article

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