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

Jin Xie, Fengzhi Yang, Man Zhang, Celine Lam, Yixue Qiao, Jia Xiao, Dongdong Zhang, Yuxuan Ge, Lei Fu*, Dongsheng Xie

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

24 Citations (Scopus)

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 ± 0.03 μM against Hela and DU-145 respectively).

Original languageEnglish
Pages (from-to)131-134
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number2
DOIs
Publication statusPublished - 2017
Externally publishedYes

Keywords

  • Antiproliferative activity
  • CAPE derivatives
  • Caffeic acid esters
  • Structure-activity relationships

Fingerprint

Dive into the research topics of 'Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety'. Together they form a unique fingerprint.

Cite this