Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety. Issue 2 (15th January 2017)

• Record Type: Journal Article
• Authors: Xie, Jin; Yang, Fengzhi; Zhang, Man; Lam, Celine; Qiao, Yixue; Xiao, Jia; Zhang, Dongdong; Ge, Yuxuan; Fu, Lei; Xie, Dongsheng
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 2(2017)
• Page Start: 131
• Page End: 134
• Publication Date: 2017-01-15
• Subjects: Caffeic acid esters -- CAPE derivatives -- Antiproliferative activity -- Structure-activity relationships; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.12.007
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: The electronic effect of 2′-substituents on CAPE's antiproliferative activity. 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).