Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety

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• 作者：Jin Xie ; Fengzhi Yang ; Man Zhang ; Celine Lam ; Yixue Qiao ; Jia Xiao ; Dongdong Zhang ; Yuxuan Ge ; Lei Fu ; ^{leifu@sjtu.edu.cn} ; Dongsheng Xie ; ^{dshxie@sjtu.edu.cn}
• 关键词：Caffeic acid esters ; CAPE derivatives ; Antiproliferative activity ; Structure-activity relationships
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：27
• 期：2
• 页码：131-134
• 全文大小：772 K
• 卷排序：27

文摘

A series of CAPE derivatives with mono-substituted phenylethanols moiety were synthesized and evaluated by MTT assay on growth of 4 human cancer cell lines (Hela, DU-145, MCF-7 and ECA-109). The substituent effects on the antiproliferative activity were systematically investigated for the first time. It was found that electron-donating and hydrophobic substituents at 2′-position of phenylethanol moiety could significantly enhance CAPE’s antiproliferative activity. 2′-Propoxyl derivative, as a novel caffeic acid ester, exhibited exquisite potency (IC50 = 0.4 ± 0.02 & 0.6 ± 0.03 μM against Hela and DU-145 respectively).