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

✍ Scribed by Leticia G. León; Rubén M. Carballo; María C. Vega-Hernández; Pedro O. Miranda; Víctor S. Martín; Juan I. Padrón; José M. Padrón

• Publisher: John Wiley and Sons
• Year: 2008
• Tongue: English
• Weight: 487 KB
• Volume: 3
• Category: Article
• ISSN: 1860-7179
• DOI: 10.1002/cmdc.200800212

✦ Synopsis

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 GI~50~ 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 G~2~/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.