Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors |
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| Authors: | Surya K De Vida Chen John L Stebbins Li-Hsing Chen Jason F Cellitti Thomas Machleidt Elisa Barile Megan Riel-Mehan Russell Dahl Li Yang Aras Emdadi Ria Murphy Maurizio Pellecchia |
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| Institution: | 1. Burnham Institute for Medical Research, La Jolla, CA 92037, USA;2. Invitrogen Corporation, Invitrogen Discovery Services, 501 Charmany Drive, Madison, WI 53719, USA |
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| 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. |
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