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

  作者 QIU XU; DU YUHONG; LOU BIN; ZUO YINGLIN; SHAO WEIYAN; HUO YINGPENG; HUANG JIANING; YU YANJUN; ZHOU BINHUA; DU JUN; FU HAIAN; BU XIANZHANG  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2010年53-23;  页码  8260-8273  
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[摘要]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-kappa B inhibition activity over the parent compound curcumin, at least in part by inhibiting I kappa B phosphorylation and degradation via IKK blockage; selected 4-arylidene curcumin analogues also reduced the tumorigenic potential of cancer cells in a clonogenic assay.

 
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