topoisomerase inhibitors


Summary: Compounds that inhibit the activity of DNA TOPOISOMERASES.

Top Publications

  1. Rahman A, Al Shakliah N, Yin W, Kadi A. In vitro Investigation of Metabolic Profiling of a Potent Topoisomerase Inhibitors Fluorescein Hydrazones (FLHs) in RLMs by LC-MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2017;1054:27-35 pubmed publisher
    Metabolic profiling of newly reported two topoisomerase inhibitors namely fluorescein hydrazones (FLHs) were studied in rat liver microsomes (RLMs) and the data were acquired in a liquid chromatography (LC) ion trap mass spectrometry...
  2. Kadi A, Al Shakliah N, Yin W, Rahman A. In vitro investigation of metabolic profiling of newly developed topoisomerase inhibitors (ethyl fluorescein hydrazones, EtFLHs) in RLMs by LC-MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2017;1054:93-104 pubmed publisher
    Metabolic profiling of newly reported five topoisomerase inhibitors namely ethyl fluorescein hydrazones (EtFLHs) were studied in rat liver microsomes (RLMs) and the data were acquired in a liquid chromatography (LC) ion trap mass ..
  3. Hajjar D, Kremb S, Sioud S, Emwas A, Voolstra C, Ravasi T. Anti-cancer agents in Saudi Arabian herbals revealed by automated high-content imaging. PLoS ONE. 2017;12:e0177316 pubmed publisher
    ..analyses of the cytological profiles of the tested compounds suggested that these plants contain possible topoisomerase inhibitors that could be effective in cancer treatment...
  4. Thapa Magar T, Kadayat T, Lee H, Park S, Bist G, Shrestha A, et al. 2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent. Bioorg Med Chem Lett. 2017;27:3279-3283 pubmed publisher
    ..A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity. ..
  5. Yuan Z, Chen S, Chen C, Chen J, Chen C, Dai Q, et al. Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy. Eur J Med Chem. 2017;138:1135-1146 pubmed publisher
    ..Our study suggested that single agents inhibiting Topo and PARP concurrently might be an alternative for cancer therapy and 11l represented a potential lead compound for development of antitumor agents. ..
  6. O Connor S. PLANT BIOCHEMISTRY. Fighting cancer while saving the mayapple. Science. 2015;349:1167-8 pubmed publisher
  7. León K, Herrera Martínez M, Ramirez Mares M, Hernandez Carlos B. EVALUATION OF ANTICANCER POTENTIAL OF EIGHT VEGETAL SPECIES FROM THE STATE OF OAXACA. Afr J Tradit Complement Altern Med. 2017;14:61-73 pubmed publisher
    ..cuspidata, A. integrifolium, G. mexicanum, and L. achyranthifolia stems showed antitopoisomerase and non-mutagenic activities, and consequently could be promising as a source of anticancer drugs. ..
  8. Paubelle E, Zylbersztejn F, Thomas X. The preclinical discovery of vosaroxin for the treatment of acute myeloid leukemia. Expert Opin Drug Discov. 2017;12:747-753 pubmed publisher
    ..Furthermore, vosaroxin also was seen to be active in multidrug-resistant preclinical models. However, further studies have to be performed to better evaluate its place in the armamentarium against AML. ..
  9. Correia S, Poeta P, Hebraud M, Capelo J, Igrejas G. Mechanisms of quinolone action and resistance: where do we stand?. J Med Microbiol. 2017;66:551-559 pubmed publisher

More Information


  1. de Oliveira J, Lima T, Vendramini Costa D, de Lacerda Pedrosa S, Lafayette E, da Silva R, et al. Thiosemicarbazones and 4-thiazolidinones indole-based derivatives: Synthesis, evaluation of antiproliferative activity, cell death mechanisms and topoisomerase inhibition assay. Eur J Med Chem. 2017;136:305-314 pubmed publisher
    ..These results demonstrate the importance of thiosemicarbazone, especially the derivative 2b, as a promising candidate for anticancer therapy. ..
  2. Mitton Fry M, Brickner S, Hamel J, Barham R, Brennan L, Casavant J, et al. Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV. Bioorg Med Chem Lett. 2017;27:3353-3358 pubmed publisher
    ..aureus strains with mutations conferring resistance to NBTIs. Compound 14 also displayed an improved hERG IC50 of 85.9?M and a favorable profile in the anesthetized guinea pig model. ..