β′-Hydroxy-α,β-unsaturated ketones: A new pharmacophore for the design of anticancer drugs

A series of β′-hydroxy-α,β-unsaturated ketones were prepared by means of an iron(III) catalyzed domino process. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, SW1573, and WiDr. The results showed that β′-hydroxy-α,β-unsaturated ketones were more potent than α,β-unsaturated ketones. The best activity profiles were obtained for the derivatives bearing cyclic or branched substituents on the side chains.

Graphical abstractThe in vitro antitumor activity of diverse α,β-unsaturated ketones is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide