Evidence map›Paper›PMID 40652414›Full record

ArticleMolecular diversity2025

Synthesis and multi-target evaluation of 2-(2-phenylethyl)/2,3-styrylchromone derivatives as potential anti-Alzheimer's disease agents.

JiaHao Lu, YingQI Qiu, ChenHao Zhao, Ai-Qun Wu, Haiou Jiang, Li-Qun Shen

Abstract read
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In one paragraph

Article in Molecular diversity, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0citing papers in PubMed
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1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

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3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

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PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors.

JiaHao LuCollege of Chemistry and Chemical Engineering, Guangxi Minzu University, Key Laboratory of Chemistry and Engineering of Forest Products, State Ethnic Affairs Commission, Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Engineering Research Center of Low-Carbon and High-Quality Utilization of Forest Biomass, University of Guangxi, Nanning, 530006, China.
YingQI QiuCollege of Chemistry and Chemical Engineering, Guangxi Minzu University, Key Laboratory of Chemistry and Engineering of Forest Products, State Ethnic Affairs Commission, Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Engineering Research Center of Low-Carbon and High-Quality Utilization of Forest Biomass, University of Guangxi, Nanning, 530006, China.
ChenHao ZhaoCollege of Chemistry and Chemical Engineering, Guangxi Minzu University, Key Laboratory of Chemistry and Engineering of Forest Products, State Ethnic Affairs Commission, Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Engineering Research Center of Low-Carbon and High-Quality Utilization of Forest Biomass, University of Guangxi, Nanning, 530006, China.
Ai-Qun WuCollege of Chemistry and Chemical Engineering, Guangxi Minzu University, Key Laboratory of Chemistry and Engineering of Forest Products, State Ethnic Affairs Commission, Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Engineering Research Center of Low-Carbon and High-Quality Utilization of Forest Biomass, University of Guangxi, Nanning, 530006, China.
Haiou JiangInstitute of Biomedicine, Hunan University of Medicine, Huaihua, 418000, China. hhjiangh@126.com.
Li-Qun ShenCollege of Chemistry and Chemical Engineering, Guangxi Minzu University, Key Laboratory of Chemistry and Engineering of Forest Products, State Ethnic Affairs Commission, Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Engineering Research Center of Low-Carbon and High-Quality Utilization of Forest Biomass, University of Guangxi, Nanning, 530006, China. liqunshen@126.com.

Funding

National Natural Science Foundation of China 21762006
6 · The paper itself

Abstract

A series of novel 2-(2-phenylethyl)chromone and 2/3-styrylchromone derivatives (A1-A16, B1-B43) were designed, synthesized, and systematically evaluated for their multi-target activities against key pathological factors of Alzheimer's disease (AD). In vitro studies demonstrated that compound B22 exhibited potent and selective acetylcholinesterase (AChE) inhibition (IC₅₀ = 2.52 ± 1.11 μM) with negligible activity against butyrylcholinesterase (BuChE) (IC₅₀ > 500 μM), along with strong monoamine oxidase-B (MAO-B) inhibition (93.6% inhibition at 1 μM). Thioflavin T (ThT) fluorescence assays revealed that B18 and B22 effectively inhibited the aggregation of both Aβ40/42 peptides (IC₅₀ = 1.44 and 1.00 μM, respectively) and Tau fibrillization (IC₅₀ = 2.61 and 3.32 μM), while promoting the disaggregation of pre-formed amyloid fibrils. Molecular docking and molecular dynamics (MD) simulations indicated that B22 exhibited favorable binding affinities (ΔG ≈ - 7.3 kcal/mol) and stable interactions within the AChE active site. Furthermore, B22 significantly attenuated reactive oxygen species (ROS) levels (by up to 89.5%) and rescued Aβ-induced cytotoxicity in SHSY5Y cells, restoring cell viability to 85.7% at 20 μM. Collectively, these results highlight chromone-based scaffolds, particularly compound B22, as promising multifunctional candidates for the development of disease-modifying therapeutics targeting AD.

Indexed as

AcetylcholinesteraseAlzheimer’s diseaseAβ40/42ChromoneTau

Identifiers

PMID40652414

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.