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

KJ Okolotowicz, R Shi, X Zheng, M MacDonald…

Index: Okolotowicz, Karl J.; Shi, Ranxin; Zheng, Xueying; MacDonald, Mary; Reed, John C.; Cashman, John R. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 5 p. 1918 - 1924

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Citation Number: 10

Abstract

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 ...