Caffeic acid phenethyl ester (CAPE)-derivatives act as selective inhibitors of acetylcholinesterase

被引：15

作者：

Giessel, Josephine M. ^{[1
]}

Loesche, Anne ^{[1
]}

Csuk, Rene ^{[1
]}

机构：

[1] Martin Luther Univ Halle Wittenberg, Organ Chem, Kurt Mothes Str 2, D-06120 Halle, Saale, Germany

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2019年 / 177卷

关键词：

Cinnamic acid phenethyl esters; Caffeic acid phenethyl ester; Acetylcholinesterase; Butyrylcholinesterase; Inhibitors; ANTIPROLIFERATIVE ACTIVITY; ANALOGS; CYTOTOXICITY; DERIVATIVES; APOPTOSIS; PROPOLIS; CAPE;

D O I：

10.1016/j.ejmech.2019.05.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Unexpected inhibitory effects against eeAChE could be found for a newly synthesized class of caffeic acid phenethyl ester (CAPE) derivatives. Thus, phenethyl-(E)-3-(3,5-dimethoxy-4-phenethoxyphenyl)-acrylate (K-i = 1.97 +/- 0.38 mu M, K-i' = 2.44 +/- 0.07 mu M) and 4-(2-(((E)-3-(3,4-bis(benzyloxy)phenyl)acryloyl)oxy)ethyl)-1,2-phenylene (2E,2'E)-bis(3-(3,4-bis(benzyloxy)phenyl)acrylate) (K-i = 0.72 +/- 0.31 mu M, K-i' = 1.80 +/- 0.21 mu M) showed very good inhibition of eeAChE, while being non cytotoxic for malignant human cancer cells and non-malignant mouse fibroblasts. Also, they are weak inhibitors for BChE (from equine serum). (C) 2019 Elsevier Masson SAS. All rights reserved.

引用

页码：259 / 268

页数：10

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