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Information × Registration Number 0219U102405, 0115U002593 , R & D reports Title Researches of mechanisms of biological activity of organic compounds in model systems popup.stage_title Head Вовк Андрій Іванович, Registration Date 28-12-2019 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description2 The subjects of the study were macrocyclic phosphonic acid derivatives, thiazole derivatives, vitamin B1, nitroxyl radicals, enzymes and other proteins as potential biological targets. As a result of the study, the mechanisms of inhibition of protein tyrosine phosphatases by phosphorylated macroheterocyclic polyamines and fullerenes were established. It has been found that sulfonylcalix[4]arene can be a promising platform for designing selective inhibitors of protein tyrosine phosphatases. Among the macrocyclic derivatives of phosphinic acids, potent and selective inhibitors of PTP1B were found. The obtained results indicate the ability of functionalized sulfonylcalix[4]arenes to selectively inhibit the activity of nucleotidepyrophosphatase/phosphodiesterase 1 in comparison to alkaline phosphatases. It was found the patterns of complexation of macrocyclic inhibitors with albumin. For the first time, the use of macrocyclic phosphonic acid derivatives of the defined structure in the photoactivation blockage of activity of glutathione-S-transferase, which is involved in cellular mechanisms of drug resistance, was proposed. New directions for the search of xanthine oxidase inhibitors among synthetic aurone derivatives have been formulated. Mechanisms of inhibition of human dihydrofolate reductase with 6-amino-5-heterylpyrimidines were substantiated. It has been found that O-acyl substituted structural analogues of thiamine can exhibit anticholinesterase activity in rat brain synaptosomes. By means of EPR method spectral characteristics of nitroxyl monoradicals and biradicals based on adamantanecarboxylic acid esters and amides as potential spin probes as well as their antioxidant properties and ability for complexation with albumin and β-cyclodextrin were established. Product Description popup.authors Buldenko Vladyslav M. Hushcha Tatiana О. Kobzar Oleksandr L. Mischenko Iryna M. Melnyk Andrii К. Mykula Mariya S. Muzychka Oxana V. Ocheretnyuk Alla D. Sukhoveev Olexandr V. Tanchuk Vsevolod Yu. Trush Viacheslav V. Shulha Yuliya O. popup.nrat_date 2020-04-02 Close