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
  • 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: [email protected].
  • 3. School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China. Electronic address: [email protected].
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.