ArticleOncotarget2017
Antivascular and antitumor properties of the tubulin-binding chalcone TUB091.
Article in Oncotarget, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed.
- Synthesis and Study of Substituted Chalcones Combined with Fluoroazobenzenes-New Photoswitches for Application in Biological Systems.Molecules (Basel, Switzerland) · 2026Article
- Synthesis of Epoxyoxirenes: Phytotoxic Activity and Enzymatic Target Identification.Plants (Basel, Switzerland) · 2025Article
- (Pharmaceuticals (Basel, Switzerland) · 2025Article
- The Anthelmintic Activity ofPathogens (Basel, Switzerland) · 2025Article
- Computational discovery of potential therapeutic agents against brain-eating amoeba (Naegleria fowleri).PloS one · 2025Article
- Identification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022Review
- Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones.International journal of molecular sciences · 2022Review
- Article
- Pharmacophore optimization of imidazole chalcones to modulate microtubule dynamics.Bioorganic chemistry · 2022Article
- Molecular interactions at the colchicine binding site in tubulin: An X-ray crystallography perspective.Drug discovery today · 2022Review
- X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.Journal of medicinal chemistry · 2021Article
- Identification of novel microtubule inhibitors effective in fission yeast and human cells and their effects on breast cancer cell lines.Open biology · 2021Article
- Anticancer activity of pyrimidodiazepines based on 2-chloro-4-anilinoquinazoline: synthesis, DNA binding and molecular docking.RSC advances · 2021Article
- Chalcone Derivatives: Role in Anticancer Therapy.Biomolecules · 2021Review
- α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer.Molecules (Basel, Switzerland) · 2021Article
- Etiology and management of hypertension in patients with cancer.Cardio-oncology (London, England) · 2021Review
- The Newly Synthetized Chalcone L1 Is Involved in the Cell Growth Inhibition, Induction of Apoptosis and Suppression of Epithelial-to-Mesenchymal Transition of HeLa Cells.Molecules (Basel, Switzerland) · 2021Article
- Angiogenesis, Anti-Tumor, and Anti-Metastatic Activity of Novel α-Substituted Hetero-Aromatic Chalcone Hybrids as Inhibitors of Microtubule Polymerization.Frontiers in chemistry · 2021Article
- Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues.MedChemComm · 2019Article
Corrections and comments
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Authors and funding
16 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We investigated the microtubule-destabilizing, vascular-targeting, anti-tumor and anti-metastatic activities of a new series of chalcones, whose prototype compound is (E)-3-(3''-amino-4''-methoxyphenyl)-1-(5'-methoxy-3',4'-methylendioxyphenyl)-2-methylprop-2-en-1-one (TUB091). X-ray crystallography showed that these chalcones bind to the colchicine site of tubulin and therefore prevent the curved-to-straight structural transition of tubulin, which is required for microtubule formation. Accordingly, TUB091 inhibited cancer and endothelial cell growth, induced G2/M phase arrest and apoptosis at 1-10 nM. In addition, TUB091 displayed vascular disrupting effects in vitro and in the chicken chorioallantoic membrane (CAM) assay at low nanomolar concentrations. A water-soluble L-Lys-L-Pro derivative of TUB091 (i.e. TUB099) showed potent antitumor activity in melanoma and breast cancer xenograft models by causing rapid intratumoral vascular shutdown and massive tumor necrosis. TUB099 also displayed anti-metastatic activity similar to that of combretastatin A4-phosphate. Our data indicate that this novel class of chalcones represents interesting lead molecules for the design of vascular disrupting agents (VDAs). Moreover, we provide evidence that our prodrug approach may be valuable for the development of anti-cancer drugs.
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