Selective benzimidazole inhibitors of the antigen receptor-mediated NF-κB activation pathway Original Research Article

Dysregulated antigen receptor-mediated NF-κB activation can contribute to development of autoimmunity, chronic inflammation, and malignancy. A chemical biology screening strategy has identified a substituted benzimidazole that selectively inhibits antigen receptor-mediated NF-κB activation without blocking other NF-κB activation pathways. A library of analogs was synthesized and the structure–activity relationship and metabolic stability for the series is presented.