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ID: ALA1139595
Journal: Bioorg Med Chem Lett
Title: Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.
Authors: Bonafoux D, Bonar S, Christine L, Clare M, Donnelly A, Guzova J, Kishore N, Lennon P, Libby A, Mathialagan S, McGhee W, Rouw S, Sommers C, Tollefson M, Tripp C, Weier R, Wolfson S, Min Y.
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-1beta stimulated rheumatoid arthritis-derived synovial fibroblasts, demonstrating their potential usefulness as NF-kappaB regulators.
CiteXplore: 15911271