β′‐Hydroxy‐α,β‐unsaturated ketones: A new pharmacophore for the design of anticancer drugs. Part 2.

Abstract

Novel antiproliferative β′‐acyloxy‐α,β ‐unsaturated ketones were obtained by means of an iron(III)‐catalyzed multicomponent domino process (ABB′ 3CR). The most active derivatives displayed GI50 values in the range of 0.5–3.9 μ M against a panel of representative human solid tumor cell lines: A2780, SW1573, HBL‐100, T‐47D and WiDr. Analysis of cells following 24 h exposure to these drugs showed cell cycle arrest in the S and G2/M phase, in a dose‐dependent manner. Our data indicate that the β ′‐acyloxy‐α,β ‐unsaturated ketones cause permanent damage to the cells and induce apoptosis.