A novel class of potent NF-kappaB signaling inhibitors

Johann Leban; Marcel Baierl; Jan Mies; Viola Trentinaglia; Sandra Rath; Kerstin Kronthaler; Kristina Wolf; Astrid Gotschlich; Markus H J Seifert

doi:10.1016/j.bmcl.2007.08.022

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.

Authors

Johann Leban¹, Marcel Baierl, Jan Mies, Viola Trentinaglia, Sandra Rath, Kerstin Kronthaler, Kristina Wolf, Astrid Gotschlich, Markus H J Seifert

Affiliation

¹ 4SC AG, Am Klopferspitz 19a, 82152 Martinsried, Germany. [email protected]

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.

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