Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNFα-induced nuclear factor-κB activation inhibition

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.

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► New biaryl-based chalcones obtained by microwave assistant Suzuki coupling involved reactions.
► The position of F substitution on C ring of title compounds affects their anticancer activity greatly.
► Electron-donating group substituted on B ring of title compounds enhance their anticancer activity.
► Amination of A ring of title compounds enhance their NF-κB inhibitory activity.
► Both activities of title compounds are generally in accordance with each other.