title: Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.
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.
authors: Sanford-Burnham Medical Research Institute, La Jolla, CA 92037, USA.
authors: Surya K
authors: SK
authors: De
authors: Elisa
authors: E
authors: Barile
authors: Vida
authors: V
authors: Chen
authors: John L
authors: JL
authors: Stebbins
authors: Jason F
authors: JF
authors: Cellitti
authors: Thomas
authors: T
authors: Machleidt
authors: Coby B
authors: CB
authors: Carlson
authors: Li
authors: L
authors: Yang
authors: Russell
authors: R
authors: Dahl
authors: Maurizio
authors: M
authors: Pellecchia
mesh_terms: D000255:Adenosine Triphosphate; D001665:Binding Sites; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D018716:Molecular Mimicry; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D013876:Thiophenes; C549318:thiophene-3-carboxylic acid; D000255:Adenosine Triphosphate; D048031:JNK Mitogen-Activated Protein Kinases