Design, synthesis and anticancer activities of stilbene-coumarin hybrid compounds: Identification of novel proapoptotic agents

详细信息    查看全文

• 作者：Federica Belluti ; Gabriele Fontana ; Laura Dal Bo ; Nives Carenini ; Chiara Giommarelli ; Franco Zunino
• 关键词：Coumarins ; Resveratrol ; Apoptosis ; Antitumor ; Hybrid compound
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：15 May 2010
• 年：2010
• 卷：18
• 期：10
• 页码：3543-3550
• 全文大小：490 K

文摘

The naturally occurring coumarins and resveratrol, attract great attention due to their wide range of biological properties, including anticancer, antileukemic, antibacterial and anti-inflammatory activities; moreover, their cancer chemopreventive property have been recently emphasized. A novel class of hybrid compounds, obtained by introducing a substituted trans-vinylbenzene moiety on a coumarin backbone, was synthesized and evaluated for the antitumor profile. A number of derivatives showed a good antiproliferative activity, in some cases higher to that of the reference compound resveratrol. The most promising compounds in this series were 14 and 17, endowed with excellent antiproliferative and proapoptotic activities. The present study suggests that the 7-methoxycoumarin nucleus, together with the 3,5-disubstitution pattern of the trans-vinylbenzene moiety, are likely promising structural features to obtain excellent antitumor compounds endowed with a apoptosis-inducing capability.