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Information × Registration Number 0223U004791, 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 04-12-2023 Organization Institute of Organic Chemistry NAS of Ukraine popup.description2  During the implementation of the Project, new types of calix[4]arenes, thiacalix[4]arenes and sulfonylcalix[4]arenes were synthesized. The obtained compounds contain pharmacophoric sulfonamide groups with alkyl substituents, fragments of five-membered or six-membered heterocycles on the upper rim of the macrocycle. Amphiphilic calix[4]arenes of cationic and anionic nature, as well as inherentlychiral calix[4]arenes with biologically active fragments of hydroxymethylphosphonic, methylenebisphosphonic or ketophosphonic acids were synthesized. Researches conducted at the V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine showed that derivatives of calix[4]arenes, thiacalix[4]arenes and sulfonylcalix[4]arenes with N,N-dialkylaminosulfonylamide groups on the calixarene upper rim can be inhibitors of protein tyrosine phosphatases, glutathione-S-transferases and malate dehydrogenase. Some representatives of calix[4]arenephosphoric, thiacalix[4]arenephosphoric, calix[4]arenephosphonic and calix[4]arenephosphinic acids were found to be micromolar and submicromolar inhibitors of protein tyrosine phosphatases and glutathione-S-transferases. According to the results of a comparative study, new micromolar and submicromolar inhibitors of protein tyrosine phosphatases, glutathione-S-transferases and cholinesterases were found among calix[4]arenes and thiacalixarenes containing sulfonamide groups on the upper rim of the macrocycle with fragments of five-membered and six-membered heterocycles. Product Description popup.authors Buldenko Vladislav Mikolajovich Vovk Andriy Ivanovich Kalchenko Vitaliy Ivanovich Kobzar Olexandr Leonidovich Selihova Anna Igorivna Cherenok Serhii Oleksijovich Shulga Yurii Vasilovich popup.nrat_date 2023-12-04 Close