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Synthesis and identification of new 4-arylidene curcumin analogues as potential anticancer agents targeting nuclear factor-?B signaling pathway.

ABSTRACT: 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-?B inhibition activity over the parent compound curcumin, at least in part by inhibiting I?B phosphorylation and degradation via IKK blockage; selected 4-arylidene curcumin analogues also reduced the tumorigenic potential of cancer cells in a clonogenic assay.

SUBMITTER: Qiu X

PROVIDER: S-EPMC3990230 | biostudies-literature | 2010 Dec

REPOSITORIES: biostudies-literature

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Synthesis and identification of new 4-arylidene curcumin analogues as potential anticancer agents targeting nuclear factor-κB signaling pathway.

Qiu Xu X Du Yuhong Y Lou Bin B Zuo Yinglin Y Shao Weiyan W Huo Yingpeng Y Huang Jianing J Yu Yanjun Y Zhou Binhua B Du Jun J Fu Haian H Bu Xianzhang X

Journal of medicinal chemistry 20101111 23

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 impr ...[more]

PMID: 21070043

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