Synthesis and Identification of New 4-Arylidene Curcumin Analogues as Potential Anticancer Agents Targeting Nuclear Factor-κB Signaling Pathway

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• 作者：Xu Qiu ; Yuhong Du ; Bin Lou ; Yinglin Zuo ; Weiyan Shao ; Yingpeng Huo ; Jianing Huang ; Yanjun Yu ; Binhua Zhou ; Jun Du ; Haian Fu ; Xianzhang Bu
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：December 9, 2010
• 年：2010
• 卷：53
• 期：23
• 页码：8260-8273
• 全文大小：1137K
• 年卷期：v.53,no.23(December 9, 2010)
• ISSN：1520-4804

文摘

A series of curcumin analogues including new 4-arylidene curcumin analogues (4-arylidene-1,7-bisarylhepta-1,6-diene-3,5-diones) were synthesized. Cell growth inhibition assays revealed that most 4-arylidene curcumin analogues can effectively decrease the growth of a panel of lung cancer cells at submicromolar and low micromolar concentrations. High content analysis technology coupled with biochemical studies showed that this new class of 4-arylidene curcumin analogues exhibits significantly improved NF-κB inhibition activity over the parent compound curcumin, at least in part by inhibiting IκB phosphorylation and degradation via IKK blockage; selected 4-arylidene curcumin analogues also reduced the tumorigenic potential of cancer cells in a clonogenic assay.