ArticleOncology reports2012
Natural chalcones as dual inhibitors of HDACs and NF-κB.
Article in Oncology reports, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
31 citing papers in PubMed, 83 citations in OpenAlex.
- Article
- Tailoring the Regioselectivity ofJournal of agricultural and food chemistry · 2025Article
- Pharmacological potential of natural chalcones: a recent studies and future perspective.Frontiers in pharmacology · 2025Review
- An Insight into Synthetic Strategies, SAR Study and Anticancer Mechanism of Chalcone Derivatives: Medicinal Chemistry Perspective.Current drug research reviews · 2025Review
- Discovery of Di(het)arylmethane and Dibenzoxanthene Derivatives as Potential Anticancer Agents.International journal of molecular sciences · 2024Article
- Multienzymatic biotransformation of flavokawain B by entomopathogenic filamentous fungi: structural modifications and pharmacological predictions.Microbial cell factories · 2024Article
- Progress in discovery and development of natural inhibitors of histone deacetylases (HDACs) as anti-cancer agents.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Isoliquiritigenin ameliorates abnormal oligodendrocyte development and behavior disorders induced by white matter injury.Frontiers in pharmacology · 2024Article
- Extracellular vesicles enhance theFrontiers in chemistry · 2024Article
- Challenges in natural product-based drug discovery assisted withRSC advances · 2023Review
- Potent Antioxidant and Anti-Tyrosinase Activity of Butein and Homobutein Probed by Molecular Kinetic and Mechanistic Studies.Antioxidants (Basel, Switzerland) · 2023Article
- Targeting histone deacetylases for cancer therapy: Trends and challenges.Acta pharmaceutica Sinica. B · 2023Review
- Chalcones and Gastrointestinal Cancers: Experimental Evidence.International journal of molecular sciences · 2023Review
- Pharmacophore optimization of imidazole chalcones to modulate microtubule dynamics.Bioorganic chemistry · 2022Article
- Chalcones: Synthetic Chemistry Follows Where Nature Leads.Biomolecules · 2021Review
- Review
- Finding New Molecular Targets of Familiar Natural Products Using In Silico Target Prediction.International journal of molecular sciences · 2020Article
- Review
- Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence.Frontiers in pharmacology · 2020Review
- Natural Chalcones in Chinese Materia Medica: Licorice.Evidence-based complementary and alternative medicine : eCAM · 2020Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Histone deacetylase enzymes (HDACs) are emerging as a promising biological target for cancer and inflammation. Using a fluorescence assay, we tested the in vitro HDAC inhibitory activity of twenty-one natural chalcones, a widespread group of natural products with well-known anti-inflammatory and antitumor effects. Since HDACs regulate the expression of the transcription factor NF-κB, we also evaluated the inhibitory potential of the compounds on NF-κB activation. Only four chalcones, isoliquiritigenin (no. 10), butein (no. 12), homobutein (no. 15) and the glycoside marein (no. 21) showed HDAC inhibitory activity with IC50 values of 60-190 µM, whereas a number of compounds inhibited TNFα-induced NF-κB activation with IC50 values in the range of 8-41 µM. Interestingly, three chalcones (nos. 10, 12 and 15) inhibited both TNFα-induced NF-κB activity and total HDAC activity of classes I, II and IV. Molecular modeling and docking studies were performed to shed light into dual activity and to draw structure-activity relationships among chalcones (nos. 1-21). To the best of our knowledge this is the first study that provides evidence for HDACs as potential drug targets for natural chalcones. The dual inhibitory potential of the selected chalcones on NF-κB and HDACs was investigated for the first time. This study demonstrates that chalcones can serve as lead compounds in the development of dual inhibitors against both targets in the treatment of inflammation and cancer.
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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.