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Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole 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. The compounds are substrate competitive inhibitors that bind to the docking site of the kinase. The reported medicinal chemistry and structure-based optimizations studies resulted in the discovery of selective and potent thiadiazole JNK inhibitors that display promising in vivo activity in mouse models of insulin insensitivity.

SUBMITTER: De SK 

PROVIDER: S-EPMC2667321 | biostudies-literature | 2009 Apr

REPOSITORIES: biostudies-literature

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Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.

De Surya K SK   Stebbins John L JL   Chen Li-Hsing LH   Riel-Mehan Megan M   Machleidt Thomas T   Dahl Russell R   Yuan Hongbin H   Emdadi Aras A   Barile Elisa E   Chen Vida V   Murphy Ria R   Pellecchia Maurizio M  

Journal of medicinal chemistry 20090401 7


We report comprehensive structure-activity relationship studies on a novel series of c-Jun N-terminal kinase (JNK) inhibitors. The compounds are substrate competitive inhibitors that bind to the docking site of the kinase. The reported medicinal chemistry and structure-based optimizations studies resulted in the discovery of selective and potent thiadiazole JNK inhibitors that display promising in vivo activity in mouse models of insulin insensitivity. ...[more]

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