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

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

  • Bioorg Med Chem. 2011 Apr 15;19(8):2582-8. doi: 10.1016/j.bmc.2011.03.017.
Surya K De 1,  Elisa Barile,  Vida Chen,  John L Stebbins,  Jason F Cellitti,  Thomas Machleidt,  Coby B Carlson,  Li Yang,  Russell Dahl,  Maurizio Pellecchia
Affiliations

Affiliation

  • 1 Sanford-Burnham Medical Research Institute, La Jolla, CA 92037, USA.
PMID: 21458276 DOI: 10.1016/j.bmc.2011.03.017
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.

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