Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNF¦Á-induced nuclear factor-¦ÊB activation inhibition

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• 作者：Yinglin Zuo ; Yi Yu ; Shuni Wang ; Weiyan Shao ; Binhua Zhou ; Li Lin ; Zhuoyu Luo ; Ruogu Huang ; Jun Du ; Xianzhang Bu ; ^{phsbxzh@mail.sysu.edu.cn}
• 关键词：Biphenyl chalcones ; Cytotoxicity ; NF-¦ÊB inhibition ; High content analysis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：April, 2012
• 年：2012
• 卷：50
• 期：Complete
• 页码：393-404
• 全文大小：788 K

文摘

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-¦ÊB (NF-¦ÊB) 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-¦ÊB nuclear translocation inhibition activities and potent compounds were found.