%0 Journal Article
%T Novel Deoxyvasicinone每Donepezil Hybrids as Potential Multitarget Drug Candidates for Alzheimer＊s Disease
%J -
%D 2019
%R https://doi.org/10.1021/acschemneuro.8b00699
%X In this study, we designed and synthesized a series of deoxyvasicinone每donepezil hybrids and determined whether they could be used as novel multitarget inhibitors for Alzheimer＊s disease. In vitro studies showed that most of the hybrids demonstrated moderate to potent inhibition of hAChE, BACE1, and A汕1每42 aggregation. In particular, the hybrids 10a, 10d, 11a, and 11j exhibited excellent inhibitory activities against hAChE (IC50 = 56.14, 5.91, 3.29, and 8.65 nM, respectively), BACE1 (IC50 = 0.834, 0.167, 0.129, and 0.085 米M, respectively), and A汕1每42 aggregation (IC50 = 13.26, 19.43, 9.26, and 5.41 米M, respectively). In addition, 10a and 11a exhibited very low cytotoxicity and showed remarkable neuroprotective activity against A汕1每42-induced damage in SH-SY5Y cells
%U https://pubs.acs.org/doi/10.1021/acschemneuro.8b00699