It is reported that up-regulation of JNK activity is associated with a number of disease states  such as type- 2 diabetes, obesity, cancer, inflammation, and stroke. Therefore, JNK inhibitors are expected to be effective therapeutic agents against a variety of  diseases. In this paper, we describe the synthesis and SAR of a novel series for bi-dentate JNK inhibitors.  Compounds are synthesized using a weak ATP mimetic coupled with a variety of JIP1 peptides. Compounds are very potent, selective sub nanomolar JNK inhibitors. These bi-dentate JNK inhibitors also showed in vivo activities in diabetes mice model.

Design, synthesis, and biological evaluation of bi-dentate c-Jun N-terminal kinase inhibitors

245th National Meeting (2013)

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