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Information × Registration Number 0217U004472, 0114U001822 , R & D reports Title New derivatives of condensed heterocyclic compounds as topoisomerase I inhibitors, antitumor agents and reagents for the detection of nucleic acids popup.stage_title Head Dubey Igor, Доктор хімічних наук Registration Date 03-02-2017 Organization Institute of Molecular Biology and Genetics of NASU popup.description2 A series of new topoisomerase I inhibitors based on poly-substituted acridines were synthesized. Among them efficient inhibitors with IC50 1.2-3.2 uM were identified. On testing in HeLa tumor cell culture compounds with antiproliferative activity were found, including those active at submicromolar concentrations (EC50 0.25-1.2 uM). The conjugates of inhibitors with polymers dextran and polyethylene glycol were obtained. Antitumor activity of CL5-dextran conjugate is 2,4 times higher than that of the free CL5 (EC50 3.4 and 8.1 uM, respectively). Parameters of the fluorescence of DNA complexes with cyanines LO were determined. Product Description popup.authors Ільченко М.М. Алексєєва І.В. Дубей Л.В. Костіна В.Г. Костенко О.М. Криворотенко Д.В. Кузів Я.Б. Негруцька В.В. popup.nrat_date 2020-04-02 Close
R & D report
New derivatives of condensed heterocyclic compounds as topoisomerase I inhibitors, antitumor agents and reagents for the detection of nucleic acids
Head: Dubey Igor. New derivatives of condensed heterocyclic compounds as topoisomerase I inhibitors, antitumor agents and reagents for the detection of nucleic acids. (popup.stage: ). Institute of Molecular Biology and Genetics of NASU. № 0217U004472
1 documents found

Updated: 2026-03-22


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