361202-25-7Relevant academic research and scientific papers
Novel IKK inhibitors: β-carbolines
Castro, Alfredo C.,Dang, Luan C.,Soucy, Francois,Grenier, Louis,Mazdiyasni, Hormoz,Hottelet, Maria,Parent, Lana,Pien, Christine,Palombella, Vito,Adams, Julian
, p. 2419 - 2422 (2003)
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.
Beta-carbolines useful for treating inflammatory disease
-
Page/Page column 85; 88, (2010/02/14)
This invention provides beta-carboline compounds of formula III-A-aa: wherein Q, G, R1, R2, R3, and R6b are as described in the specification. The compounds are useful for treating diseases such as inflammatory diseases and cancer.
Synthesis of C-14-labeled novel IKK inhibitor: 2-[14C]-N-(6- chloro-9H-pyrido [3,4-b]indol-8-yl)-3-pyridinecarboxamide
Li, Yuexian,Prakash, Shimoga R.
, p. 323 - 330 (2007/10/03)
2-[14C]-N-(6-Chloro-9H-pyrido [3,4-b]indol-8-yl)-3- pyridinecarboxamide (9A, also referred to as [14C]-PS-1145) was synthesized from [14C]-paraformaldehyde in five steps in an overall radiochemical yield of 15%. The key intermediate 1-[14C]-6-chloro-1, 2,3,4-tetrahydro-β-carboline was obtained by Pictet-Spengler cyclization of chlorotryptamine with [14C]-paraformaldehyde. Similar reactions were conducted with tryptamine to address the generality of the methodology. Copyright
Substituted beta-carbolines
-
Page 17, (2010/01/31)
Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of IκB kinase is involved.
