ArticleBioorganic & medicinal chemistry letters2016
Inhibition of human DNA topoisomerase IIα by two novel ellipticine derivatives.
Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 39 citations in OpenAlex.
- Acridine BasedMolecules (Basel, Switzerland) · 2022Article
- The Chemotherapeutic Potentials of Compounds Isolated from the Plant, Marine, Fungus, and Microorganism: Their Mechanism of Action and Prospects.Journal of tropical medicine · 2022Review
- DNA topoisomerases as molecular targets for anticancer drugs.Journal of enzyme inhibition and medicinal chemistry · 2020Review
- Selected ellipticine derivatives, known to target topoisomerase II, suppress the alternative lengthening of telomere (ALT) pathway in telomerase-negative cells.Journal of cancer research and clinical oncology · 2020Article
- Repurposing Ellipticine Hydrochloride to Combat Colistin-Resistant Extraintestinal PathogenicFrontiers in microbiology · 2020Article
- Modeling the Antileukemia Activity of Ellipticine-Related Compounds: QSAR and Molecular Docking Study.Molecules (Basel, Switzerland) · 2019Article
- 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
- Application of hepatic cytochrome bToxicology and applied pharmacology · 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
- N-thioalkylcarbazoles derivatives as new anti-proliferative agents: synthesis, characterisation and molecular mechanism evaluation.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Increasing the distance between two monomers of topoisomerase IIβ under the action of antitumor agent 4β-sulfur-(benzimidazole) 4'-demethylepipodophyllotoxin.Scientific reports · 2018Article
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Authors and funding
6 authors at 4 institutions in 2 countries.
Funding
Abstract
Ellipticine (5,11-dimethyl-6H-pyrido[4,3-b]carbazole) is an antineoplastic agent that intercalates into DNA and alters topoisomerase II activity. Unfortunately, this compound displays a number of adverse properties. Therefore, to investigate new ellipticine-based compounds for their potential as topoisomerase II-targeted drugs, we synthesized two novel derivatives, N-methyl-5-demethyl ellipticine (ET-1) and 2-methyl-N-methyl-5-demethyl ellipticinium iodide (ET-2). As determined by DNA decatenation and cleavage assays, ET-1 and ET-2 act as catalytic inhibitors of human topoisomerase IIα and are both more potent than the parent compound. Neither compound impairs the ability of the type II enzyme to bind its DNA substrate. Finally, the potency of ET-1 and ET-2 as catalytic inhibitors of topoisomerase IIα appears to be related to their ability to intercalate into the double helix.
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