On January 15, 2010, Stewart, Scott G.; Braun, Carlos J.; Ng, Sze-Ling; Polomska, Marta E.; Karimi, Mahdad; Abraham, Lawrence J. published an article.Electric Literature of 1216805-11-6 The title of the article was New thalidomide analogues derived through Sonogashira or Suzuki reactions and their TNF expression inhibition profiles. And the article contained the following:
A library of new thalidomide C4/5 analogs containing either a Ph or alkyne tether were synthesized using Sonogashira or Suzuki cross coupling reactions from their aryl halogenated precursors. All thalidomide analogs were tested for their ability to inhibit the expression of the proinflammatory cytokine Tumor Necrosis Factor (TNF). More explicitly the use of a novel reporter system utilizing the promoter region of the TNF gene in a human T-cell line provided a rapid and effective measure of NFκB transcriptional activity. Several compounds either containing either an aryl-iso-Bu or aryl-isopropoxy group were the most effective in inhibiting TNF expression, and were several times more active than thalidomide itself. Five of the more active derivatives indicated an apoptotic response while one of these compounds, containing an aldehyde tether, showed possible influence of cell cycling effects. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Electric Literature of 1216805-11-6
The Article related to structure thalidomide analog preparation tnf inhibition cancer, Pharmacology: Structure-Activity and other aspects.Electric Literature of 1216805-11-6
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