Novel 4-(4-substituted amidobenzyl)furan-2(5H)-one derivatives as topoisomerase I inhibitors

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• 作者：Cheng-Kang Peng¹ ; Ting Zeng¹ ; Xing-Jun Xu ; Yi-Qun Chang ; Wen Hou ; Kuo Lu ; Hui Lin ; Ping-Hua Sun ; Jing Lin ; ^{linjing_jnu@163.com} ; Wei-Min Chen ; ^{twmchen@jnu.edu.cn}
• 关键词：Furan-2(5H)-one ; α ; β-unsaturated lactones ; Topoisomerase I ; Antitumor
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：187-199
• 全文大小：2057 K
• 卷排序：127

文摘

Two series of 4-(4-substituted amido-benzyl)furan-2(5H)-one derivatives were synthesized. Compounds bearing an exocyclic double bond showed significant Topo I inhibitory and potent anti-proliferative activity. Dual action mechanisms were identified for this class of compounds.