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J Med Chem. 2010 Dec 9;53(23):8260-73. doi: 10.1021/jm1004545. Epub 2010 Nov 11.

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

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  • 1School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510275, China.

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-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.

PMID:
21070043
[PubMed - indexed for MEDLINE]
PMCID:
PMC3990230
Free PMC Article

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