title: Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.
abstract: A series of thiadiazole derivatives has been designed as potential allosteric, substrate competitive inhibitors of the protein kinase JNK. We report on the synthesis, characterization and evaluation of a series of compounds that resulted in the identification of potent and selective JNK inhibitors targeting its JIP-1 docking site.
authors.affiliation: Burnham Institute for Medical Research, La Jolla, CA 92037, USA.
authors.forename: Surya K
authors.initials: SK
authors.lastname: De
authors.forename: Vida
authors.initials: V
authors.lastname: Chen
authors.forename: John L
authors.initials: JL
authors.lastname: Stebbins
authors.forename: Li-Hsing
authors.initials: LH
authors.lastname: Chen
authors.forename: Jason F
authors.initials: JF
authors.lastname: Cellitti
authors.forename: Thomas
authors.initials: T
authors.lastname: Machleidt
authors.forename: Elisa
authors.initials: E
authors.lastname: Barile
authors.forename: Megan
authors.initials: M
authors.lastname: Riel-Mehan
authors.forename: Russell
authors.initials: R
authors.lastname: Dahl
authors.forename: Li
authors.initials: L
authors.lastname: Yang
authors.forename: Aras
authors.initials: A
authors.lastname: Emdadi
authors.forename: Ria
authors.initials: R
authors.lastname: Murphy
authors.forename: Maurizio
authors.initials: M
authors.lastname: Pellecchia
mesh_terms: D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D013830:Thiadiazoles; D048031:JNK Mitogen-Activated Protein Kinases