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
