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Registration Number

0220U101516, 0115U001404 , R & D reports

Title

Development of the system of fast screening of DNA-binding compounds for the search of inhibitors of nucleic acids biosynthesis enzymes as potential antitumor and antimicrobial agents

Head

Dubey Igor Ya., Доктор хімічних наук

Registration Date

12-02-2020

Organization

Institute of Molecular Biology and Genetics of NAS of Ukraine

Description

New DNA ligands were synthesized and their interact5ion with duplex and quadruplex DNA was studied. Upon testing in enzymatic test-systems based on topoisomerase I and telomerase active inhibitors were found with IC50 in the range 0,2-5 uM. Interaction of some inhibitors with various foorms of DNA was investigated by quantum-chemical methods, structures and energetic parameters of complexes were calculated. Study of biological activity of inhibitors revealed compounds with antiproliferative activity in HeLa tumor cell culture at low micro- and nanomolar concentrations (ЕС50 0,4-0,9 uM). Antibacterial activity of a series of topoisomerase I inhibitors against Gram-positive (Bacillus subtilis) and Gram-negative (Pseudomonas fluorescens) microorganisms was investigated. One of cyanines in 10 uM concentration showed high inhibitory activity against B.subtilis; at 50 uM bacteriostatic activity demonstrated also three acridine derivatives.  

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