Du_2020_Bioorg.Med.Chem.Lett__127659

Reference

Title : Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation - Du_2020_Bioorg.Med.Chem.Lett__127659
Author(s) : Du H , Jiang X , Ma M , Xu H , Liu S , Ma F
Ref : Bioorganic & Medicinal Chemistry Lett , :127659 , 2020
Abstract :

A novel series of deoxyvasicinone-tetrahydro-beta-carboline hybrids were synthesized and evaluated as acetylcholinesterase (AChE) and beta-amyloid peptide (Abeta) aggregation inhibitors for the treatment of Alzheimer's disease. The results revealed that the derivatives had multifunctional profiles, including AChE inhibition, Abeta(1-42) aggregation inhibition, and neuroprotective properties. Inspiringly, hybrids 8b and 8d displayed excellent inhibitory activities against hAChE (IC(50) = 0.93 and 1.08 nM, respectively) and Abeta(1-42) self-aggregation (IC(50) = 19.71 and 2.05 M, respectively). In addition, 8b and 8d showed low cytotoxicity and good neuroprotective activity against Abeta(1-42)-induced damage in SH-SY5Y cells.

PubMedSearch : Du_2020_Bioorg.Med.Chem.Lett__127659
PubMedID: 33137375

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Citations formats

Du H, Jiang X, Ma M, Xu H, Liu S, Ma F (2020)
Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation
Bioorganic & Medicinal Chemistry Lett :127659

Du H, Jiang X, Ma M, Xu H, Liu S, Ma F (2020)
Bioorganic & Medicinal Chemistry Lett :127659