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+/-0.38muM, Ki =2.44+/-0.07muM) 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+/-0.31muM, Ki =1.80+/-0.21muM) 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).
Giessel JM, Loesche A, Csuk R (2019) Caffeic acid phenethyl ester (CAPE)-derivatives act as selective inhibitors of acetylcholinesterase Eur Journal of Medicinal Chemistry177: 259-268
Giessel JM, Loesche A, Csuk R (2019) Eur Journal of Medicinal Chemistry177: 259-268