ArticleJournal of medicinal chemistry2012
Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
21 citing papers in PubMed.
- Catalyst-Free Spontaneous Aza-Mannich/Lactamization Cascade Reaction: Easy Access to Polycyclic δ-Lactams.Molecules (Basel, Switzerland) · 2025Article
- Design, Synthesis and Bioactive Evaluation of Topo I/Molecules (Basel, Switzerland) · 2025Article
- Evaluating the indotecan-neutropenia relationship in patients with solid tumors by population pharmacokinetic modeling and sigmoidal ECancer chemotherapy and pharmacology · 2023Article
- Review
- Article
- Trifluoroethanol Promoted Castagnoli-Cushman Cycloadditions of Imines with Homophthalic Anhydride.Molecules (Basel, Switzerland) · 2022Article
- Indenoisoquinoline Topoisomerase Inhibitors Strongly Bind and Stabilize theJournal of the American Chemical Society · 2019Article
- Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors.Molecular cancer therapeutics · 2018Article
- Formal [4 + 2] cycloaddition of imines with alkoxyisocoumarins.Organic & biomolecular chemistry · 2018Article
- Characterization and structure-activity relationships of indenoisoquinoline-derived topoisomerase I inhibitors in unsilencing the dormantMolecular autism · 2018Article
- Stereochemistry and Reactivity of the HPA-Imine Mannich Intermediate.Tetrahedron letters · 2017Article
- 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
- Design, Synthesis, and Biological Evaluation of Potential Prodrugs Related to the Experimental Anticancer Agent Indotecan (LMP400).Journal of medicinal chemistry · 2016Article
- Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.Bioorganic & medicinal chemistry · 2016Article
- Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a new pair of resistance-associated mutations.Journal of experimental & clinical cancer research : CR · 2016Article
- Synthesis of indolo[4,3-Synthetic communications · 2016Article
- Inhibitory Effect of the Noncamptothecin Topoisomerase I Inhibitor LMP-400 on Female Mice Models and Human Pheochromocytoma Cells.Endocrinology · 2015Article
- Plasma pharmacokinetics of the indenoisoquinoline topoisomerase I inhibitor, NSC 743400, in rats and dogs.Cancer chemotherapy and pharmacology · 2015Article
- Synthesis and biological evaluation of nitrated 7-, 8-, 9-, and 10-hydroxyindenoisoquinolines as potential dual topoisomerase I (Top1)-tyrosyl-DNA phosphodiesterase I (TDP1) inhibitors.Journal of medicinal chemistry · 2015Article
- Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.Journal of medicinal chemistry · 2014Article
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Authors and funding
9 authors.
Funding
Abstract
Hydroxylated analogues of the anticancer topoisomerase I (Top1) inhibitors indotecan (LMP400) and indimitecan (LMP776) have been prepared because (1) a variety of potent Top1 poisons are known that contain strategically placed hydroxyl groups, which provides a clear rationale for incorporating them in the present case, and (2) the hydroxylated compounds could conceivably serve as synthetic standards for the identification of metabolites. Indeed, incubating LMP400 and LMP776 with human liver microsomes resulted in two major metabolites of each drug, which had HPLC retention times and mass fragmentation patterns identical to those of the synthetic standards. The hydroxylated indotecan and indimitecan metabolites and analogues were tested as Top1 poisons and for antiproliferative activity in a variety of human cancer cell cultures and in general were found to be very potent. Differences in activity resulting from the placement of the hydroxyl group are explained by molecular modeling analyses.
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