Document Detail


Synthesis and identification of new 4-arylidene curcumin analogues as potential anticancer agents targeting nuclear factor-κB signaling pathway.
MedLine Citation:
PMID:  21070043     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Xu Qiu; Yuhong Du; Bin Lou; Yinglin Zuo; Weiyan Shao; Yingpeng Huo; Jianing Huang; Yanjun Yu; Binhua Zhou; Jun Du; Haian Fu; Xianzhang Bu
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2010-11-11
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  53     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2014-02-04     Completed Date:  2014-04-15     Revised Date:  2014-04-18    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  8260-73     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology
Cell Line, Tumor
Cell Nucleus / metabolism
Curcumin / analogs & derivatives*,  chemical synthesis,  pharmacology
Humans
Inhibitory Concentration 50
Lung Neoplasms / pathology
Magnetic Resonance Spectroscopy
NF-kappa B / metabolism*
Signal Transduction / drug effects*
Tumor Necrosis Factor-alpha / antagonists & inhibitors
Grant Support
ID/Acronym/Agency:
P01 CA116676/CA/NCI NIH HHS; P01CA116676/CA/NCI NIH HHS; P50 CA128613/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/NF-kappa B; 0/Tumor Necrosis Factor-alpha; IT942ZTH98/Curcumin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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