- A novel class of potent NF-kappaB signaling inhibitors.
A novel class of potent NF-kappaB signaling inhibitors.
Bioorganic & medicinal chemistry letters (2007-09-18)
Johann Leban, Marcel Baierl, Jan Mies, Viola Trentinaglia, Sandra Rath, Kerstin Kronthaler, Kristina Wolf, Astrid Gotschlich, Markus H J Seifert
PMID17869512
RÉSUMÉ
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.
MATÉRIAUX