fragrant alkane acyl tetrahydro-β-Carboline and its derivatives in the treatment of metabolic diseases
The present invention discloses an aromatic alkanoyl tetrahydro-beta-carboline compound represented by a structural formula (I), and related analogs thereof or hydrates or pharmaceutically acceptable salts thereof, and the application of the compound or p
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Paragraph 0110
(2017/01/31)
Novel IKK inhibitors: β-carbolines
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 activation of NF-κB in whole cells, as well as blocking TNF-α release in LPS-challenged mice.