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. Epub 2007 Aug 15.

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.

MeSH terms

  • Cell Proliferation / drug effects
  • NF-kappa B / antagonists & inhibitors*
  • NF-kappa B / metabolism
  • Quantitative Structure-Activity Relationship
  • Signal Transduction / drug effects*

Substances

  • NF-kappa B