Synthesis and Structure Activity Relationship Studies of Benzothieno [3, 2-b] furan Derivatives as a Novel Class of IKK. BETA. Inhibitors

H Sugiyama, M Yoshida, K Mori, T Kawamoto…

文献索引：Sugiyama, Hideyuki; Yoshida, Masato; Mori, Kouji; Kawamoto, Tomohiro; Sogabe, Satoshi; Takagi, Terufumi; Oki, Hideyuki; Tanaka, Toshimasa; Kimura, Hiroyuki; Ikeura, Yoshinori Chemical and Pharmaceutical Bulletin, 2007 , vol. 55, # 4 p. 613 - 624

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被引用次数: 28

摘要

As a novel class of IKKβ inhibitors, a series of tricyclic furan derivatives was designed and synthesized based on the structure of known thiophene IKKβ inhibitors. Among the various fused furan derivatives synthesized, a benzothieno [3, 2-b] furan derivative 13a displayed potent inhibitory activity towards IKKβ in enzymatic and cellular assays. The potent inhibitory activity originates from an intramolecular non-bonded S… O interaction which was ...