A novel class of potent NF-kappaB signaling inhibitors

  • Bioorg Med Chem Lett. 2007 Nov 1;17(21):5858-62. doi: 10.1016/j.bmcl.2007.08.022.
Johann Leban  1 ,  Marcel Baierl ,  Jan Mies ,  Viola Trentinaglia ,  Sandra Rath ,  Kerstin Kronthaler ,  Kristina Wolf ,  Astrid Gotschlich ,  Markus H J Seifert
Affiliations
PMID: 17869512 DOI: 10.1016/j.bmcl.2007.08.022
Abstract

A novel class of NF-kappaB pathway signaling inhibitors was discovered by virtual screening, medicinal chemistry, and QSAR analysis. An initial set of compounds inhibited NF-kappaB signaling in a whole cell reporter gene assay in the micro-molar range. Activity was improved step by step by medicinal chemistry to yield nano-molar signaling inhibitors.