ArticleJournal of medicinal chemistry2014
Synthesis and biological evaluation of new carbohydrate-substituted indenoisoquinoline topoisomerase I inhibitors and improved syntheses of the experimental anticancer agents indotecan (LMP400) and indimitecan (LMP776).
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Divergent synthesis of indenoisoquinolines and indenoisochromenes by rhodium-catalysed cyclocondensation ofRSC advances · 2026Article
- Imidazole Hybrids: A Privileged Class of Heterocycles in Medicinal Chemistry with New Insights into Anticancer Activity.Molecules (Basel, Switzerland) · 2025Review
- Synthesis and Biological Activity of a New Indenoisoquinoline Copper Derivative as a Topoisomerase I Inhibitor.International journal of molecular sciences · 2023Article
- Review
- A Novel Copper(II) Indenoisoquinoline Complex Inhibits Topoisomerase I, Induces G2 Phase Arrest, and Autophagy in Three Adenocarcinomas.Frontiers in oncology · 2022Article
- Epigenetic modulation and apoptotic induction by a novel imidazo-benzamide derivative in human lung adenocarcinoma cells.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2021Article
- Proteins from the DNA Damage Response: Regulation, Dysfunction, and Anticancer Strategies.Cancers · 2021Review
- Article
- Benefits and applications of microwave-assisted synthesis of nitrogen containing heterocycles in medicinal chemistry.RSC advances · 2020Review
- Indenoisoquinoline Topoisomerase Inhibitors Strongly Bind and Stabilize theJournal of the American Chemical Society · 2019Article
- Article
- Characterization and structure-activity relationships of indenoisoquinoline-derived topoisomerase I inhibitors in unsilencing the dormantMolecular autism · 2018Article
- Imidazoles as potential anticancer agents.MedChemComm · 2017Review
- Clinical and pharmacologic evaluation of two dosing schedules of indotecan (LMP400), a novel indenoisoquinoline, in patients with advanced solid tumors.Cancer chemotherapy and pharmacology · 2016Article
- Investigation of the Structure-Activity Relationships of Aza-A-Ring Indenoisoquinoline Topoisomerase I Poisons.Journal of medicinal chemistry · 2016Article
- Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.Bioorganic & medicinal chemistry · 2016Article
- Indenopyrans - synthesis and photoluminescence properties.Beilstein journal of organic chemistry · 2016Article
- Synthesis of indolo[4,3-Synthetic communications · 2016Article
- Single-Molecule Supercoil Relaxation Assay as a Screening Tool to Determine the Mechanism and Efficacy of Human Topoisomerase IB Inhibitors.Molecular cancer therapeutics · 2015Article
- Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.Journal of medicinal chemistry · 2015Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Carbohydrate moieties were strategically transported from the indolocarbazole topoisomerase I (Top1) inhibitor class to the indenoisoquinoline system in search of structurally novel and potent Top1 inhibitors. The syntheses and biological evaluation of 20 new indenoisoquinolines glycosylated with linear and cyclic sugar moieties are reported. Aromatic ring substitution with 2,3-dimethoxy-8,9-methylenedioxy or 3-nitro groups exerted strong effects on antiproliferative and Top1 inhibitory activities. While the length of the carbohydrate side chain clearly correlated with antiproliferative activity, the relationship between stereochemistry and biological activity was less clearly defined. Twelve of the new indenoisoquinolines exhibit Top1 inhibitory activity equal to or better than that of camptothecin. An advanced synthetic intermediate from this study was also used to efficiently prepare indotecan (LMP400) and indimitecan (LMP776), two anticancer agents currently under investigation in a Phase I clinical trial at the National Institutes of Health.
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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.