A novel class of potent NF-kappaB signaling inhibitors.
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.
Leban
Johann
J
4SC AG, Am Klopferspitz 19a, 82152 Martinsried, Germany. leban@4sc.com
Baierl
Marcel
M
Mies
Jan
J
Trentinaglia
Viola
V
Rath
Sandra
S
Kronthaler
Kerstin
K
Wolf
Kristina
K
Gotschlich
Astrid
A
Seifert
Markus H J
MH
D049109:Cell Proliferation / Q000187:drug effects; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D021281:Quantitative Structure-Activity Relationship; D015398:Signal Transduction / Q000187:drug effects*
D016328:NF-kappa B