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Information × Registration Number 0221U105925, 0120U103978 , R & D reports Title Design, synthesis and activity of calixarene derivatives as inhibitors of protein tyrosine phosphatases and other enzymes popup.stage_title Head Kalchenko Vitaly I., Доктор хімічних наук Registration Date 13-09-2021 Organization Institute of Organic Chemistry NAS of Ukraine popup.description2 The properties of new calix[4arenephosphoric, calix[4]arephosphonic and calix[4]arephosphinic acids as inhibitors of therapeutically important isoforms of glutathione-S-transferase and protein phosphatases were synthesized and studied, the relationship between the structure and activity of inhibitors in vitro has been established, and possible mechanisms of inhibition have been proposed. The characteristics of glutathione-S-transferase inhibition by methylene bisphosphonate and α-hydroxy-methylene bisphosphonate derivatives of calix[4]arenes with lipophilic substituents at the lower rim have been justified for the first time. Based on the structure-dependent activity of macrocyclic inhibitors,the glutathione-S-transferase has been identified as a possible target for calix[4]arephosphinic acids. It is shown that the properties of the studied calix[4]arephosphorus compounds in the process of biological transport may provide the formation of complexes with human serum albumin. The results of a comparative study of calixarenephosphoric and calixarenephosphinic acids with respect to protein tyrosine phosphatases and glutathione-S-transferase allow us to make assumptions about the properties of these compounds as dual-acting inhibitors. Product Description popup.authors Buldenko Vladyslav M. Vovk Andriy Ivanovych Kalchenko Vitaly Ivanovich Kobzar Oleksandr L. Trybrat Olexandr O Cherenok Sergiy Olexijovich Shulga Yuriy V popup.nrat_date 2021-09-13 Close