ArticleJournal of medicinal chemistry2012
Chemical modification of the multitarget neuroprotective compound fisetin.
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 44 papers, 1 of them a synthesis that pooled it.
What it found
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Who cites it
44 citing papers in PubMed, 1 synthesis or guideline pooled it, 98 citations in OpenAlex.
- The Neuroprotective Role of Fisetin in Different Neurological Diseases: a Systematic Review.Molecular neurobiology · 2023Pooled it
- Fisetin Attenuates Amyloid-Beta-Induced Neurotoxicity in Human Neuroblastoma SH-SY5Y Cells: Integrating In Silico Target Prediction and In Vitro Validation.Journal of biochemical and molecular toxicology · 2026Article
- Ferroptosis and hearing loss: from molecular mechanisms to therapeutic interventions.Journal of enzyme inhibition and medicinal chemistry · 2025Review
- Fisetin Mitigates Chronic Lung Injury Induced by Benzo(a)Pyrene by Regulation of Inflammation and Oxidative Stress.Current issues in molecular biology · 2025Article
- Fisetin as a chemoprotective and chemotherapeutic agent: mechanistic insights and future directions in cancer therapy.Medical oncology (Northwood, London, England) · 2025Review
- The Role of AMP-activated Protein Kinase in Oxytosis/Ferroptosis: Protector or Potentiator?Antioxidants & redox signaling · 2024Review
- CMS121 Partially Attenuates Disease Progression in Mouse Models of Huntington's Disease.Molecular neurobiology · 2024Article
- Mechanochemical Approach to Obtaining a Multicomponent Fisetin Delivery System Improving Its Solubility and Biological Activity.International journal of molecular sciences · 2024Article
- A plant flavonol and genetic suppressors rescue a pathogenic mutation associated with kinesin in neurons.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Article
- Review
- Attenuation of Age-Related Hearing Impairment in Senescence-Accelerated Mouse Prone 8 (SAMP8) Mice Treated with Fatty Acid Synthase Inhibitor CMS121.Journal of molecular neuroscience : MN · 2023Article
- Flavonols in Action: Targeting Oxidative Stress and Neuroinflammation in Major Depressive Disorder.International journal of molecular sciences · 2023Review
- The Geroprotective Drug Candidate CMS121 Alleviates Diabetes, Liver Inflammation, and Renal Damage in db/db Leptin Receptor Deficient Mice.International journal of molecular sciences · 2023Article
- Fisetin in Cancer: Attributes, Developmental Aspects, and Nanotherapeutics.Pharmaceuticals (Basel, Switzerland) · 2023Review
- NiRSC advances · 2022Article
- The search for anti-oxytotic/ferroptotic compounds in the plant world.British journal of pharmacology · 2021Review
- Defining a pharmacological inhibitor fingerprint for oxytosis/ferroptosis.Free radical biology & medicine · 2021Article
- Natural products targeting mitochondria: emerging therapeutics for age-associated neurological disorders.Pharmacology & therapeutics · 2021Review
- Protective effect of fisetin against subchronic chlorpyrifos-induced toxicity on oxidative stress biomarkers and neurobehavioral parameters in adult male albino mice.Toxicological research · 2021Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Many factors are implicated in age-related central nervous system (CNS) disorders, making it unlikely that modulating only a single factor will provide effective treatment. Perhaps a better approach is to identify small molecules that have multiple biological activities relevant to the maintenance of brain function. Recently, we identified an orally active, neuroprotective, and cognition-enhancing molecule, the flavonoid fisetin, that is effective in several animal models of CNS disorders. Fisetin has direct antioxidant activity and can also increase the intracellular levels of glutathione (GSH), the major endogenous antioxidant. In addition, fisetin has both neurotrophic and anti-inflammatory activity. However, its relatively high EC(50) in cell based assays, low lipophilicity, high topological polar surface area (tPSA), and poor bioavailability suggest that there is room for medicinal chemical improvement. Here we describe a multitiered approach to screening that has allowed us to identify fisetin derivatives with significantly enhanced activity in an in vitro neuroprotection model while at the same time maintaining other key activities.
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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.