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. 2017 Jan 15;27(2):131-134.
doi: 10.1016/j.bmcl.2016.12.007. Epub 2016 Dec 5.

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

Jin Xie  1 , Fengzhi Yang  1 , Man Zhang  1 , Celine Lam  1 , Yixue Qiao  1 , Jia Xiao  1 , Dongdong Zhang  1 , Yuxuan Ge  1 , Lei Fu  2 , Dongsheng Xie  3
Affiliations

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

Jin Xie et al. Bioorg Med Chem Lett. .

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).

Keywords: Antiproliferative activity; CAPE derivatives; Caffeic acid esters; Structure-activity relationships.

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