含单取代苯乙醇部分的咖啡酸酯的抗增殖活性及构效关系
Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety.
作者信息
Xie Jin, Yang Fengzhi, Zhang Man, Lam Celine, Qiao Yixue, Xiao Jia, Zhang Dongdong, Ge Yuxuan, Fu Lei, Xie Dongsheng
机构信息
School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
出版信息
Bioorg Med Chem Lett. 2017 Jan 15;27(2):131-134. doi: 10.1016/j.bmcl.2016.12.007. Epub 2016 Dec 5.
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 (IC=0.4±0.02 & 0.6±0.03μM against Hela and DU-145 respectively).
合成了一系列带有单取代苯乙醇部分的咖啡酸苯乙酯（CAPE）衍生物，并通过MTT法对4种人类癌细胞系（Hela、DU-145、MCF-7和ECA-109）的生长进行了评估。首次系统研究了取代基对其抗增殖活性的影响。结果发现，苯乙醇部分2'-位的供电子和疏水取代基可显著增强CAPE的抗增殖活性。2'-丙氧基衍生物作为一种新型咖啡酸酯，表现出优异的活性（对Hela和DU-145的IC50分别为0.4±0.02和0.6±0.03μM）。
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