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Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides

2005; Elsevier BV; Volume: 15; Issue: 11 Linguagem: Inglês

10.1016/j.bmcl.2005.03.090

1464-3405

D. Bonafoux, Sheri L. Bonar, Lori J. Christine, Michael Clare, Ann M. Donnelly, Julia A. Guzova, Nandini Kishore, Patrick J. Lennon, Adam H. Libby, Sumathy Mathialagan, William E. McGhee, Sharon Rouw, Cindy Sommers, Michael B. Tollefson, Catherine S. Tripp, Richard M. Weier, Serge G. Wolfson, Min Yao,

Immune Response and Inflammation

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.