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Caffeic Acid Phenethyl Ester (CAPE)-derivatives Act as Selective Inhibitors of Acetylcholinesterase

Caffeic Acid Phenethyl Ester (CAPE)-derivatives Act as Selective Inhibitors of Acetylcholinesterase

Josephine M Gießel, Anne Loesche, René Csuk, Immo Serbian

Eur J Med Chem. 2019 Sep 1;177:259-268.

PMID: 31158743

Abstract:

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 (Ki = 1.97 ± 0.38 μM, Ki´ = 2.44 ± 0.07 μM) 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) (Ki = 0.72 ± 0.31 μM, Ki´ = 1.80 ± 0.21 μM) 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).

Chemicals Related in the Paper:

Catalog Number	Product Name	CAS Number	Price
AP104594709	Caffeic acid phenethyl ester	104594-70-9	Price
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LS7931098	3-(Benzyloxy)-6-bromo-2-fluorophenylboronic acid		Price
LS7931201	2,4-bis(benzyloxy)pyrimidine-5-boronic acid		Price

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