2. Academic Validation
  3. Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety

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

  • Bioorg Med Chem Lett. 2017 Jan 15;27(2):131-134. doi: 10.1016/j.bmcl.2016.12.007.
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

Affiliations

  • 1 School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
  • 2 School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China. Electronic address: leifu@sjtu.edu.cn.
  • 3 School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China. Electronic address: dshxie@sjtu.edu.cn.
PMID: 27979593 DOI: 10.1016/j.bmcl.2016.12.007
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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