447427-82-9Relevant articles and documents
Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase
De, Surya K.,Barile, Elisa,Chen, Vida,Stebbins, John L.,Cellitti, Jason F.,MacHleidt, Thomas,Carlson, Coby B.,Yang, Li,Dahl, Russell,Pellecchia, Maurizio
supporting information; experimental part, p. 2582 - 2588 (2011/05/17)
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.