title: Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNFα-induced nuclear factor-κB activation inhibition.
abstract: 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-κB (NF-κB) 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-κB nuclear translocation inhibition activities and potent compounds were found.
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, XinGang Xi Road 135#, GuangZhou 510006, People's Republic of China.
authors.forename: Yinglin
authors.initials: Y
authors.lastname: Zuo
authors.forename: Yi
authors.initials: Y
authors.lastname: Yu
authors.forename: Shuni
authors.initials: S
authors.lastname: Wang
authors.forename: Weiyan
authors.initials: W
authors.lastname: Shao
authors.forename: Binhua
authors.initials: B
authors.lastname: Zhou
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.forename: Zhuoyu
authors.initials: Z
authors.lastname: Luo
authors.forename: Ruogu
authors.initials: R
authors.lastname: Huang
authors.forename: Jun
authors.initials: J
authors.lastname: Du
authors.forename: Xianzhang
authors.initials: X
authors.lastname: Bu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D021381:Protein Transport / Q000187:drug effects; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha