Simple di- and trivanillates exhibit cytostatic properties toward cancer cells resistant to pro-apoptotic stimuli

详细信息    查看全文

• 作者：Delphine Lamoral-Theys ; Laurent Pottier ; Fré ; dé ; ric Kerff ; Franç ; ois Dufrasne ; Fabien Proutiè ; re ; Nathalie Wauthoz ; Philippe Neven ; Laurent Ingrassia ; Pierre Van Antwerpen ; Florence Le
• 关键词：Polyphenol ; Kinase ; Cancer ; Apoptosis resistance ; Cytostatic activity
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：1 June 2010
• 年：2010
• 卷：18
• 期：11
• 页码：3823-3833
• 全文大小：765 K

文摘

A series of 33 novel divanillates and trivanillates were synthesized and found to possess promising cytostatic rather than cytotoxic properties. Several compounds under study decreased by >50 % the activity of Aurora A, B, and C, and WEE1 kinase activity at concentrations <10 % of their IC₅₀ growth inhibitory ones, accounting, at least partly, for their cytostatic effects in cancer cells and to a lesser extent in normal cells. Compounds 6b and 13c represent interesting starting points for the development of cytostatic agents to combat cancers, which are naturally resistant to pro-apoptotic stimuli, including metastatic malignancies.