ArticleMolecules (Basel, Switzerland)2012
Inhibitory evaluation of sulfonamide chalcones on β-secretase and acylcholinesterase.
Article in Molecules (Basel, Switzerland), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 51 citations in OpenAlex.
- Recent advances towards BACE1 drug discovery and therapeutics design.RSC medicinal chemistry · 2026Review
- Pharmacological potential of natural chalcones: a recent studies and future perspective.Frontiers in pharmacology · 2025Review
- Flavonoid and Chalcone Scaffolds as Inhibitors of BACE1: Recent Updates.Combinatorial chemistry & high throughput screening · 2024Review
- New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties.International journal of molecular sciences · 2023Article
- Bioassay-Guided Alkaloids Isolation fromMolecules (Basel, Switzerland) · 2023Article
- Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors.International journal of molecular sciences · 2022Review
- Synthesis, Structural and Biological Properties of the Ring-A Sulfonamido Substituted Chalcones: A Review.Molecules (Basel, Switzerland) · 2021Review
- A Comprehensive Review of Aminochalcones.Molecules (Basel, Switzerland) · 2020Review
- Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of SomeMolecules (Basel, Switzerland) · 2020Article
- Exploring Biological Activity of 4-Oxo-4Biomolecules · 2019Article
- In Vitro Evaluation and Docking Studies of 5-oxo-5International journal of molecular sciences · 2019Article
- Inhibitory Effects of Novel 7-Substituted 6-iodo-3-Molecules (Basel, Switzerland) · 2019Article
- Novel chalcone derivatives containing a 1,2,4-triazine moiety: design, synthesis, antibacterial and antiviral activities.RSC advances · 2019Article
- Pharmaceutical and medicinal significance of sulfur (SEuropean journal of medicinal chemistry · 2019Review
- Small Multitarget Molecules Incorporating the Enone Moiety.Molecules (Basel, Switzerland) · 2019Article
- Synthesis and Evaluation of the 4-Substituted 2-Hydroxy-5-Iodochalcones and Their 7-Substituted 6-Iodoflavonol Derivatives for Inhibitory Effect on Cholinesterases and β-Secretase.International journal of molecular sciences · 2018Article
- Anti-Amyloid Aggregation Activity of Black Sesame Pigment: Toward a Novel Alzheimer's Disease Preventive Agent.Molecules (Basel, Switzerland) · 2018Article
- Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2017Article
- Synthesis, Biological Evaluation and Molecular Modelling of 2'-Hydroxychalcones as Acetylcholinesterase Inhibitors.Molecules (Basel, Switzerland) · 2016Article
- Diverse Molecular Targets for Chalcones with Varied Bioactivities.Medicinal chemistry · 2015Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The action of β-secretase (BACE1) is strongly correlated with the onset of Alzheimer's disease (AD). Aminochalcone derivatives were examined for their ability to inhibit BACE1. Parent aminochalcones showed two digit micromolar IC(50)s against BACE1. Potency was enhanced 10-fold or more by introducing benzenesulfonyl derivatives to the amino group: 1 (IC(50) = 48.2 μM) versus 4a (IC(50) = 1.44 μM) and 2 (IC(50) = 17.7 μM) versus 5a (IC(50) = 0.21 μM). The activity was significantly influenced by position and number of hydroxyl groups on the chalcone B-ring: 3,4-dihydroxy 5a (IC(50) = 0.21 μM) > 4-hydroxy 4a (IC(50) = 1.44 μM) > 2,4-dihydroxy 6 (IC(50) = 3.60 μM) > 2,5-dihydroxy 7 (IC(50) = 16.87 μM) > des hydroxy 4b (IC(50) = 168.7 μM). Lineweaver-Burk and Dixon plots and their secondary replots indicate that compound 5a was a mixed inhibitor with reversible and time-dependent behavior. Potent BACE1 inhibitors 4a,c,f, 5a-c showed moderate inhibition against two other enzymes implicated in AD pathogenesis, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC(50)s ranging between 56.1 ~ 95.8 μM and 19.5 ~ 79.0 μM, respectively.
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Registered trials
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.