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Information × Registration Number 0224U001883, 0122U001220 , R & D reports Title Synthesis of N,O,S-containing heterocycles and study of their interaction with nucleic acids popup.stage_title Head Okovytyi Serhii І., Доктор хімічних наук Registration Date 01-02-2024 Organization Oles Honchar Dnipro National University popup.description2  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 popup.authors Borysenko Iryna O. Gaponov Olexandr O. Dil Kateryna V. Kovalenko Serhii I. Okovytyy Serhii I. Palchykov Vitalii O. Pylypenko Olena O. Shtemenko Nataliia I. popup.nrat_date 2024-02-01 Close