ArticleBioorganic & medicinal chemistry2016
Hydroxylated chalcones with dual properties: Xanthine oxidase inhibitors and radical scavengers.
Article in Bioorganic & medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 90 citations in OpenAlex.
- Article
- Advances in Xanthine Oxidase Inhibition: A Review of Potential Bioactive Synthetic Compounds.Archiv der Pharmazie · 2025Review
- Research Progress on Phytochemicals from Mulberry with Neuroprotective Effects: A Review.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Synthesis, molecular docking, assessment of biological and anti-diabetic properties of benzalacetophenone derivatives.Scientific reports · 2025Article
- Article
- Chalcones as Emerging Antibacterial Scaffolds: A Mini Review.Mini reviews in medicinal chemistry · 2025Review
- Xanthine oxidase inhibition study of isolated secondary metabolites fromSaudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Article
- Recent Advances in Xanthine Oxidase Inhibitors.Mini reviews in medicinal chemistry · 2024Review
- Past, present and future of xanthine oxidase inhibitors: design strategies, structural and pharmacological insights, patents and clinical trials.RSC medicinal chemistry · 2023Review
- Synthesis of Quinazolin-2,4,6-triamine Derivatives as Non-purine Xanthine Oxidase Inhibitors and Exploration of Their Toxicological Potential.ChemMedChem · 2023Article
- Finding a Novel Chalcone-Cinnamic Acid Chimeric Compound with Antiproliferative Activity against MCF-7 Cell Line Using a Free-Wilson Type Approach.Molecules (Basel, Switzerland) · 2023Article
- Review
- Investigation on the Synthesis, Application and Structural Features of Heteroaryl 1,2-Diketones.ACS omega · 2022Article
- Insights into Intra-Tumoral Heterogeneity: Transcriptional Profiling of Chemoresistant MPM Cell Subpopulations Reveals Involvement of NFkB and DNA Repair Pathways and Contributes a Prognostic Signature.International journal of molecular sciences · 2021Article
- Curcumin-Coumarin Hybrid Analogues as Multitarget Agents in Neurodegenerative Disorders.Molecules (Basel, Switzerland) · 2021Article
- Design and development of innovative microparticulate/nanoparticulate inhalable dry powders of a novel synthetic trifluorinated chalcone derivative and Nrf2 agonist.Scientific reports · 2020Article
- Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of SomeMolecules (Basel, Switzerland) · 2020Article
- From Xanthine Oxidase Inhibition toEvidence-based complementary and alternative medicine : eCAM · 2020Review
- An Improved Method for the Synthesis of Butein Using SOClMolecules (Basel, Switzerland) · 2019Article
- Synthesis and characterization of CAPE derivatives as xanthine oxidase inhibitors with radical scavenging properties.Bioorganic chemistry · 2019Article
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
In this study, we evaluated the abilities of a series of chalcones to inhibit the activity of the enzyme xanthine oxidase (XO) and to scavenge radicals. 20 mono- and polyhydroxylated chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and then tested for inhibitory potency against XO, a known generator of reactive oxygen species (ROS). In parallel, the ability of the synthesized chalcones to scavenge a stable radical was determined. Structure-activity relationship analysis in conjunction with molecular docking indicated that the most active XO inhibitors carried a minimum of three hydroxyl groups. Moreover, the most effective radical scavengers had two neighboring hydroxyl groups on at least one of the two phenyl rings. Since it has been proposed previously that XO inhibition and radical scavenging could be useful properties for reduction of ROS-levels in tissue, we determined the chalcones' effects to rescue neurons subjected to ROS-induced stress created by the addition of β-amyloid peptide. Best protection was provided by chalcones that combined good inhibitory potency with high radical scavenging ability in a single molecule, an observation that points to a potential therapeutic value of this compound class.
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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.