Multitarget Biological Profiling of New Naphthoquinone and Anthraquinone-Based Derivatives for the Treatment of Alzheimer's Disease.

ABSTRACT: Two series of naphthoquinone and anthraquinone derivatives decorated with an aromatic/heteroaromatic chain have been synthesized and evaluated as potential promiscuous agents capable of targeting different factors playing a key role in Alzheimer's disease (AD) pathogenesis. On the basis of the in vitro biological profiling, most of them exhibited a significant ability to inhibit amyloid aggregation, PHF6 tau sequence aggregation, acetylcholinesterase (AChE), and monoamine oxidase (MAO) B. In particular, naphthoquinone 2 resulted as one of the best performing multitarget-directed ligand (MTDL) experiencing a high potency profile in inhibiting β-amyloid (Aβ₄₀) aggregation (IC₅₀ = 3.2 μM), PHF6 tau fragment (91% at 10 μM), AChE enzyme (IC₅₀ = 9.2

SUBMITTER: Campora M 

PROVIDER: S-EPMC7880572 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature