ArticleBioorganic & medicinal chemistry letters2017
Novel xanthone-polyamine conjugates as catalytic inhibitors of human topoisomerase IIα.
Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 23 citations in OpenAlex.
- Crescent-Shaped Xanthone-Benzimidazole Conjugates as New Target Probes for Telomeric G‑Quadruplex DNA and Specific Cytotoxicity on Cancer Cells.ACS pharmacology & translational science · 2025Article
- Tetrahydropyrido[4,3-d]pyrimidines as a new active scaffold for human topoisomerase II inhibitors.Scientific reports · 2025Article
- Polyamine-Drug Conjugates: Do They Boost Drug Activity?Molecules (Basel, Switzerland) · 2023Review
- An Update on the Anticancer Activity of Xanthone Derivatives: A Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Review
- Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β.Journal of medicinal chemistry · 2020Article
- Design, Synthesis, Dynamic Docking, Biochemical Characterization, andJournal of medicinal chemistry · 2020Article
- Smoothed Potential MD Simulations for Dissociation Kinetics of Etoposide To Unravel Isoform Specificity in Targeting Human Topoisomerase II.Journal of chemical information and modeling · 2019Article
- D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity.BioMed research international · 2019Article
- Novel Bacterial Topoisomerase Inhibitors Exploit Asp83 and the Intrinsic Flexibility of the DNA Gyrase Binding Site.International journal of molecular sciences · 2018Article
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Authors and funding
8 authors at 5 institutions in 3 countries.
Funding
Abstract
It has been proposed that xanthone derivatives with anticancer potential act as topoisomerase II inhibitors because they interfere with the ability of the enzyme to bind its ATP cofactor. In order to further characterize xanthone mechanism and generate compounds with potential as anticancer drugs, we synthesized a series of derivatives in which position 3 was substituted with different polyamine chains. As determined by DNA relaxation and decatenation assays, the resulting compounds are potent topoisomerase IIα inhibitors. Although xanthone derivatives inhibit topoisomerase IIα-catalyzed ATP hydrolysis, mechanistic studies indicate that they do not act at the ATPase site. Rather, they appear to function by blocking the ability of DNA to stimulate ATP hydrolysis. On the basis of activity, competition, and modeling studies, we propose that xanthones interact with the DNA cleavage/ligation active site of topoisomerase IIα and inhibit the catalytic activity of the enzyme by interfering with the DNA strand passage step.
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Registered trials
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