期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 -, 页码 393-404出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.02.023
关键词
Biphenyl chalcones; Cytotoxicity; NF-kappa B inhibition; High content analysis
资金
- National High-tech RD 863 Program [2008AA02Z304]
- National Nature Science Foundation of China [30973619, 81172931]
- Fundamental Research Funds for the Central Universities of China [09ykpy66]
A series of biaryl-based chalcones were designed as a combination of the natural chalcone and biphenyl moieties, and synthesized by two step chemistry involving Knoevenagel reaction and microwave assistant Suzuki coupling. Sulforhodamine B (SRB) assay was performed to evaluate the cell viability inhibitory abilities of these compounds against five cancer cell lines (A549, CNE2, SW480, MCF-7, and HepG2) from different tissues. Their Nuclear Factor-kappa B (NF-kappa B) nuclear translocation inhibitory activities were further investigated by High Content Analysis (HCA) based assay. Most of the compounds showed moderate to strong anticancer and NF-kappa B nuclear translocation inhibition activities and potent compounds were found. (C) 2012 Elsevier Masson SAS. All rights reserved.
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