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Inhibition of Protein Kinase C-driven Nuclear factor-kappaB Activation: Synthesis, Structure-Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules

Inhibition of Protein Kinase C-driven Nuclear factor-kappaB Activation: Synthesis, Structure-Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules

Satyamaheshwar Peddibhotla, Ranxin Shi, Pasha Khan, Layton H Smith, Arianna Mangravita-Novo, Michael Vicchiarelli, Ying Su, Karl J Okolotowicz, John R Cashman, John C Reed, Gregory P Roth

J Med Chem. 2010 Jun 24;53(12):4793-7.

PMID: 20481485

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP758679979	CID2858522		758679-97-9	Price

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