Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors

A series of quinoxalinylurea-based inhibitors are synthesized and shown to be the novel and potent inhibitors against Jnk Stimulatory Phosphatase-1 (JSP-1), which is a special member of dual-specificity protein phosphatase (DSP) family. Biological assay and computational modeling studies showed the compounds were reversible and noncompetitive inhibitors of JSP-1. JSP-1 inhibitors may be useful for the treatment of inflammatory, vascular, neurodegenerative, metabolic, and oncological diseases in humans associated with dysfunctional Jnk signaling.

Graphical abstractA series of quinoxalinylurea-based inhibitors are synthesized and shown to be the novel and potent inhibitors against JSP-1. Compound A17 showed the most potent activity to inhibit JSP-1.Figure optionsDownload full-size imageDownload as PowerPoint slide