Paper Report for: 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 H, Jiang X, Ma M, Xu H, Liu S, Ma F Ref: Bioorganic & Medicinal Chemistry Lett, :127659, 2020 : PubMed
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.
        
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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
Du H, Jiang X, Ma M, Xu H, Liu S, Ma F (2020) Bioorganic & Medicinal Chemistry Lett