Novel IKK inhibitors: β-carbolines

…, L Grenier, H Mazdiyasni, M Hottelet, L Parent…

Index: Castro, Alfredo C.; Dang, Luan C.; Soucy, Francois; Grenier, Louis; Mazdiyasni, Hormoz; Hottelet, Maria; Parent, Lana; Pien, Christine; Palombella, Vito; Adams, Julian Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 14 p. 2419 - 2422

Full Text: HTML

Citation Number: 201

Abstract

Inhibitors of IκB kinase (IKK) have long been sought as specific regulators of NF-κB. A screening effort of the endogenous IKK complex allowed us to identify 5-bromo-6-methoxy-β- carboline as a nonspecific IKK inhibitor. Optimization of this β-carboline natural product derivative resulted in a novel class of selective IKK inhibitors with IC50s in the nanomolar range. In addition, we show that one of these β-carboline analogues inhibits the ...