| Literature DB >> 27979593 |
Jin Xie1, Fengzhi Yang1, Man Zhang1, Celine Lam1, Yixue Qiao1, Jia Xiao1, Dongdong Zhang1, Yuxuan Ge1, Lei Fu2, Dongsheng Xie3.
Abstract
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±0.03μM against Hela and DU-145 respectively).Entities:
Keywords: Antiproliferative activity; CAPE derivatives; Caffeic acid esters; Structure-activity relationships
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Year: 2016 PMID： 27979593 DOI： 10.1016/j.bmcl.2016.12.007
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823