Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives

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• 作者：Silvia Serra ; Andrea Chicca ; Giovanna Delogu ; Saleta V¨¢zquez-Rodr¨ªguez ; Lourdes Santana ; Eugenio Uriarte ; Laura Casu ; J¨¹rg Gertsch
• 关键词：4-Oxycoumarins ; MCF-7 ; HL-60 ; U937 ; Neuro2a ; Cytotoxic activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 September, 2012
• 年：2012
• 卷：22
• 期：18
• 页码：5791-5794
• 全文大小：560 K

文摘

Coumarins are a large family of natural and synthetic compounds exerting different pharmacological effects, including cytotoxic, anti-inflammatory or antimicrobial. In the present communication we report the synthesis of a series of 12 diversely substituted 4-oxycoumarin derivatives including methoxy substituted 4-hydroxycoumarins, methyl, methoxy or unsubstituted 3-aryl-4-hydroxycoumarins and 4-benzyloxycoumarins and their anti-proliferative effects on breast adenocarcinoma cells (MCF-7), human promyelocytic leukemia cells (HL-60), human histiocytic lymphoma cells (U937) and mouse neuroblastoma cells (Neuro2a). The most potent bioactive molecule was the 4-hydroxy-5,7-dimethoxycoumarin (compound 1) which showed similar potency (IC₅₀ 0.2-2 ¦ÌM) in all cancer cell lines tested. This non-natural product reveals a simple bioactive scaffold which may be exploited in further studies.