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

doi:10.1016/j.bmcl.2016.12.007

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

Shanghai Jiao Tong University

Research output: Contribution to journal › Article › peer-review

28 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 language	English
Pages (from-to)	131-134
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	27
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2016.12.007
Publication status	Published - 2017
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antiproliferative activity
CAPE derivatives
Caffeic acid esters
Structure-activity relationships

Access to Document

10.1016/j.bmcl.2016.12.007

Cite this

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title = "Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety",

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).",

keywords = "Antiproliferative activity, CAPE derivatives, Caffeic acid esters, Structure-activity relationships",

author = "Jin Xie and Fengzhi Yang and Man Zhang and Celine Lam and Yixue Qiao and Jia Xiao and Dongdong Zhang and Yuxuan Ge and Lei Fu and Dongsheng Xie",

note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Ltd",

year = "2017",

doi = "10.1016/j.bmcl.2016.12.007",

language = "English",

volume = "27",

pages = "131--134",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

number = "2",

}

TY - JOUR

T1 - Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety

AU - Xie, Jin

AU - Yang, Fengzhi

AU - Zhang, Man

AU - Lam, Celine

AU - Qiao, Yixue

AU - Xiao, Jia

AU - Zhang, Dongdong

AU - Ge, Yuxuan

AU - Fu, Lei

AU - Xie, Dongsheng

PY - 2017

Y1 - 2017

N2 - 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).

AB - 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).

KW - Antiproliferative activity

KW - CAPE derivatives

KW - Caffeic acid esters

KW - Structure-activity relationships

UR - https://www.scopus.com/pages/publications/85006860810

U2 - 10.1016/j.bmcl.2016.12.007

DO - 10.1016/j.bmcl.2016.12.007

M3 - Article

C2 - 27979593

AN - SCOPUS:85006860810

SN - 0960-894X

VL - 27

SP - 131

EP - 134

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 2

ER -

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

Abstract

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Keywords

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