| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376009 | Bioorganic & Medicinal Chemistry Letters | 2005 | 6 Pages |
Abstract
A series of 21 novel 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides were synthesized and evaluated for the inhibition of IKK-2. In spite of their often modest activity on the enzyme, six selected analogs showed significant inhibition of the production of inflammatory cytokine IL-8 in IL-1β stimulated rheumatoid arthritis-derived synovial fibroblasts, demonstrating their potential usefulness as NF-κB regulators.
Graphical abstractA series of 21 novel 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides were synthesized and evaluated for the inhibition of IKK-2.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
![Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides](/preview/png/1376009.png "First Page Preview: Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides")
Authors
Dominique Bonafoux, Sheri Bonar, Lori Christine, Michael Clare, Ann Donnelly, Julia Guzova, Nandini Kishore, Patrick Lennon, Adam Libby, Sumathy Mathialagan, William McGhee, Sharon Rouw, Cindy Sommers, Michael Tollefson, Catherine Tripp, Richard Weier,