ArticleBioorganic chemistry2021
Synthesis, inverse docking-assisted identification and in vitro biological characterization of Flavonol-based analogs of fisetin as c-Kit, CDK2 and mTOR inhibitors against melanoma and non-melanoma skin cancers.
Article in Bioorganic chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 33 citations in OpenAlex.
- Computational and Experimental Analysis ofMolecules (Basel, Switzerland) · 2026Article
- Novel 2-substituted benzothiazole derivatives: synthesis,RSC advances · 2025Article
- Study on the Mechanism of Fisetin Exerting Anti-Liver Cancer Effects by Regulating Neutrophil Extracellular Traps.Food science & nutrition · 2025Article
- Structure-Photoreactivity Relationship Study of Substituted 3-Hydroxyflavones and 3-Hydroxyflavothiones for Improving Carbon Monoxide Photorelease.The Journal of organic chemistry · 2024Article
- Natural Modulators of Key Signaling Pathways in Skin Inflammageing.Clinical, cosmetic and investigational dermatology · 2024Review
- Synthesis,Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Binding interactions of hydrophobically-modified flavonols with β-glucosidase: fluorescence spectroscopy and molecular modelling study.RSC advances · 2023Article
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- A Concise Review of the Recent Structural Explorations of Chromones as MAO-B Inhibitors: Update from 2017 to 2023.Pharmaceuticals (Basel, Switzerland) · 2023Review
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- Reconstruction of the cell pseudo-space from single-cell RNA sequencing data with scSpace.Nature communications · 2023Article
- Standardized Pomegranate (PomellaMolecules (Basel, Switzerland) · 2022Article
- A review on the role of cyclin dependent kinases in cancers.Cancer cell international · 2022Review
- Dual targeting of mTOR/IL-17A and autophagy by fisetin alleviates psoriasis-like skin inflammation.Frontiers in immunology · 2022Article
- Synthesis of aspirin-curcumin mimic conjugates of potential antitumor and anti-SARS-CoV-2 properties.Bioorganic chemistry · 2021Article
- Identification of new fisetin analogs as kinase inhibitors: Data on synthesis and anti-skin cancer activities evaluation.Data in brief · 2021Article
- Fisetin is a selective adenosine triphosphate-competitive inhibitor for mitogen-activated protein kinase kinase 4 to inhibit lipopolysaccharide-stimulated inflammation.BioFactors (Oxford, England)Article
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Authors and funding
17 authors at 6 institutions in 2 countries.
Funding
Abstract
Due to hurdles, including resistance, adverse effects, and poor bioavailability, among others linked with existing therapies, there is an urgent unmet need to devise new, safe, and more effective treatment modalities for skin cancers. Herein, a series of flavonol-based derivatives of fisetin, a plant-based flavonoid identified as an anti-tumorigenic agent targeting the mammalian targets of rapamycin (mTOR)-regulated pathways, were synthesized and fully characterized. New potential inhibitors of receptor tyrosine kinases (c-KITs), cyclin-dependent kinase-2 (CDK2), and mTOR, representing attractive therapeutic targets for melanoma and non-melanoma skin cancers (NMSCs) treatment, were identified using inverse-docking, in vitro kinase activity and various cell-based anticancer screening assays. Eleven compounds exhibited significant inhibitory activities greater than the parent molecule against four human skin cancer cell lines, including melanoma (A375 and SK-Mel-28) and NMSCs (A431 and UWBCC1), with IC
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