Novel IKK inhibitors: β-carbolines

  title={Novel IKK inhibitors: $\beta$-carbolines},
  author={Alfredo C. Castro and L. C. Dang and F. Soucy and L. Grenier and H. Mazdiyasni and M. Hottelet and L. Parent and C. Pien and V. Palombella and J. Adams},
  journal={Bioorganic \& Medicinal Chemistry Letters},
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 phosphorylation of IκBα and subsequent… Expand

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