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Information × Registration Number 0216U003975, 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 03-03-2016 Organization Institute of molecular biology & genetics popup.description2 A series of new topoisomerase I inhibitors based on acridines were synthesized. The study of their biological activity in vitro revealed efficient inhibitors with ІС50 1,1-1,6 uM. A number of inhibitors were tested in tumor cell culture U87MG (glioma), and compounds with antiproliferative activity at 0,8-5 uM concentration were found. Their DNA binding constants were determined. DNA interaction parameters were found for the cyanines of LO series, including complex dissociation constants and binding energies (dG), which suggest highly affine interactions. A significant role of ionic interactions in binding process was shown. 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
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 & genetics. № 0216U003975
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Updated: 2026-03-23