ArticleJournal of medicinal chemistry2012
A synthetic chalcone as a potent inducer of glutathione biosynthesis.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 55 citations in OpenAlex.
- Apple oil as a source of ursolic acid for the treatment of hyperpigmentary disorders with molecular and clinical evaluation.Scientific reports · 2025Trial
- Discovery and Optimization of a Series of Vinyl Sulfoximine-Based Analogues as Potent Nrf2 Activators for the Treatment of Multiple Sclerosis.Journal of medicinal chemistry · 2024Article
- Synthesis and photophysical properties of novel bis-quinolin-3-yl-chalcones.RSC advances · 2024Article
- Synthesis of Bis-Chalcones and Evaluation of Its Effect on Peroxide-Induced Cell Death and Lipopolysaccharide-Induced Cytokine Production.Molecules (Basel, Switzerland) · 2023Article
- Chalcone-Derived Nrf2 Activator Protects Cognitive Function via Maintaining Neuronal Redox Status.Antioxidants (Basel, Switzerland) · 2021Article
- Chalcones: Synthetic Chemistry Follows Where Nature Leads.Biomolecules · 2021Review
- Chalcone Derivatives: Role in Anticancer Therapy.Biomolecules · 2021Review
- Chalcone derivatives: synthesis,Heliyon · 2019Article
- Design and development of Nrf2 modulators for cancer chemoprevention and therapy: a review.Drug design, development and therapy · 2018Review
- Post-translational Activation of Glutamate Cysteine Ligase with Dimercaprol: A NOVEL MECHANISM OF INHIBITING NEUROINFLAMMATIONThe Journal of biological chemistry · 2017Article
- Synthesis and cytotoxic evaluation of alkoxylated chalcones.Molecules (Basel, Switzerland) · 2014Article
- 4-methoxychalcone enhances cisplatin-induced oxidative stress and cytotoxicity by inhibiting the Nrf2/ARE-mediated defense mechanism in A549 lung cancer cells.Molecules and cells · 2013Article
- Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: critical role of methoxylation in both inhibition potency and cytotoxicity.Journal of medicinal chemistry · 2012Article
Corrections and comments
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Authors and funding
9 authors at 8 institutions in 2 countries.
Funding
Abstract
Chalcones continue to attract considerable interest due to their anti-inflammatory and antiangiogenic properties. We recently reported the ability of 2',5'-dihydroxychalcone (2',5'-DHC) to induce both breast cancer resistance protein-mediated export of glutathione (GSH) and c-Jun N-terminal kinase-mediated increased intracellular GSH levels. Herein, we report a structure-activity relationship study of a series of 30 synthetic chalcone derivatives with hydroxyl, methoxyl, and halogen (F and Cl) substituents and their ability to increase intracellular GSH levels. This effect was drastically improved with one or two electrowithdrawing groups on phenyl ring B and up to three methoxyl and/or hydroxyl groups on phenyl ring A. The optimal structure, 2-chloro-4',6'-dimethoxy-2'-hydroxychalcone, induced both a potent NF-E2-related factor 2-mediated transcriptional response and an increased formation of glutamate cysteine ligase holoenzyme, as shown using a human breast cancer cell line stably expressing a luciferase reporter gene driven by antioxidant response elements.
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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.