2. Academic Validation
  3. A novel class of potent NF-kappaB signaling inhibitors

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

Affiliation

  • 1 4SC AG, Am Klopferspitz 19a, 82152 Martinsried, Germany. leban@4sc.com
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.

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