Registration Number
0224U001883,
0122U001220
, R & D reports
Title
Synthesis of N,O,S-containing heterocycles and study of their interaction with nucleic acids
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Head
Okovytyi Serhii І., Доктор хімічних наук
Registration Date
01-02-2024
Organization
Oles Honchar Dnipro National University
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Object of research - in silico and in vitro studies, modification and synthesis of N,O,S-heterocycles, ligands, dirhenium complexes, interaction with DNA and macrophages.
The aim of the work is the targeted creation of new nucleotide-binding substances (ligands) in the series of N,O,S-heterocyclic compounds, synthesis of rhenium complexes, and study of their possible further use in medical practice. Methods for the synthesis of new 2-(3-R-1,2,4-triazol-5-yl)anilines by nucleophilic cleavage of s-triazolo[c]quinazolines as effective ligands for the creation of complexes with rhenium have been developed. Theoretical (molecular docking) and experimental in vitro studies of the antitumor activity of 2-(3-R-1,2,4-triazol-5-yl)-anilines were carried out and it was found that these compounds have a high affinity for tyrosine kinase receptors (EGFR and RET) and effectively inhibit non-small cell lung cancer cell lines. A number of new ligands were synthesized by fusing alicyclic compounds with various pharmacophore fragments. Cis-tetrachlorotetrabenzimidazole dirhenium(III) chloride and tetrabenzimidazole dioxorenium(IV) were synthesized, the structure and spectral characteristics of these complexes were studied. The interaction of cis-tetrachlorotetrabenzimidazolium dirhenium(III) chloride and tetrabenzimidazolium dioxorenium(IV) with ckit1 G4 DNA was investigated and their high efficiency was shown. The field of application is combinatorial and medicinal chemistry.
Product Description
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Borysenko Iryna O.
Gaponov Olexandr O.
Dil Kateryna V.
Kovalenko Serhii I.
Okovytyy Serhii I.
Palchykov Vitalii O.
Pylypenko Olena O.
Shtemenko Nataliia I.
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2024-02-01
