Document Report Card

ID: ALA1177698

Journal: J Med Chem

Title: Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules.

Authors: Peddibhotla S, Shi R, Khan P, Smith LH, Mangravita-Novo A, Vicchiarelli M, Su Y, Okolotowicz KJ, Cashman JR, Reed JC, Roth GP.

Abstract: A unique series of biologically active chemical probes that selectively inhibit NF-kappaB activation induced by protein kinase C (PKC) pathway activators have been identified through a cell-based phenotypic reporter gene assay. These 2-aminobenzimidazoles represent initial chemical tools to be used in gaining further understanding on the cellular mechanisms driven by B and T cell antigen receptors. Starting from the founding member of this chemical series 1a (notated in PubChem as CID-2858522), we report the chemical synthesis, SAR studies, and pharmacological profiling of this pathway-selective inhibitor of NF-kappaB activation.

CiteXplore: 20481485

DOI: 10.1021/jm1000248