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Information × Registration Number 0225U000172, (0122U000439) , R & D reports Title Synthesis and evaluation of antitumor activity of new heterocyclic and organophosphorus compounds popup.stage_title Одержання нових азагетероциклів з фармакофорними сірковмісними замісниками та їх тестування на протиракову активність. Розробка підходів до синтезу трициклічних систем з фрагментом піридопіримідину. Синтез біологічно активних молекул на основі амінокислот (серіну, цистеїну та глутаміну). Конструювання нових гетероциклічних сполук як потенційних протипухлинних агентів. Head Vovk Andrii І., д.х.н. Registration Date 06-01-2025 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description1 Development of methods for the synthesis of new heterocyclic and organophosphorus compounds, study of their properties in silico and in vitro in model systems and search and identification of substances with antitumor activity. popup.description2 The ability of (furan-2-ylmethylene)thiazolo[3,2-b][1,2,4]triazol-6(5H)-one derivatives to irreversibly inhibit glutathione-S-transferases A1-1, P1-1, as well as enzymes from horse liver and human placenta upon UV irradiation was established for the first time. The features of the effect of the inhibitors depending on their structure were demonstrated. The kinetics of glutathione-S-transferase inactivation under the action of (furan-2-ylmethylene)thiazolo[3,2-b][1,2,4]triazol-6(5H)-one derivatives was characterized by first- and second-order rate constants. Mechanisms of the photodependent transformations in the presence of (furan-2-ylmethylene)thiazolo[3,2-b][1,2,4]triazol-6(5H)-ones may involve modification of the enzyme amino acid residues essential for catalysis. Preparative methods for the synthesis of new phosphorylated azoles were developed and their in vitro biotesting was carried out on various model lines of malignant cells. The interaction of 5-formylpyrimidines with aminopyrazoles was studied. Chiral synthetic blocks based on aminophosphonate derivatives were synthesized, methods of obtaining new phosphorus analogues of natural compounds were developed. Prediction of bioactivity was carried out and new synthetic inhibitors of therapeutically important enzymes were studied. Product Description popup.authors Іvanova Іryna V. Biletskyi Ihor І. Bahrieieva Oksana S. Beiko Alona V. Bodachivskyi Yurii S. Volodymyr S. Brovarets Brusnakov Mykhailo Yu. Buldenko Vladyslav M. Verves Yevhenii V. Vydzhak Roman M. Vovk Andrii І. Herasymov Yehor S. Holovchenko Oleksandr V. Hryshkun Yevhen V. Demydchuk Bohdan A. Zhyrnov Viktor V. Zaporozhets Dmytro V. Ziabriev Volodymyr S. Kachaieva Maryna V. Kachkovskyi Oleksii D. Kobzar Oleksandr L. Kozachenko Oleksandr P. Kolodiazhna Anastasiia O. Kolodiazhna Olha O. Kolodiazhnyi Oleh I. Konovalenko Artem S. Kornii Yurii Ye. Kucher Oleksandr V. Los Oleksandr V. Liutenko Nataliia V. Mitiukhin Оleh P. Malets Yehor S. Myshko Andrii S. Moskvina Viktoriia S. Mruh Halyna P. Muzychka Liubov V. Muzychka Oksana V. Pilo Stepan H. Panchyshyn Svitlana Ya. Porkhun Svitlana V. Potikha Liudmyla M. Prisyajnyuk Dmytro V. Prokopenko Volodymyr M. Prostota Yaroslav O. Rayenko Yevhen H. Rybakova Antonina V. Severin Oleksandr O. Synenko Vitalii O. Smolii Oleh B. Solomiannyi Roman M. Sukhovieiev Oleksandr V. Tanchuk Vsevolod Yu. Mykhaylo S. Frasyniuk Chumachenko Svitlana A. Shablykin Oleh V. Shablykina Olha V. Sheiko Serhii Yu. Shulha Yrii V. Yaremchuk Iryna O. popup.nrat_date 2025-01-06 Close