Search academic texts

Information × Registration Number 0221U000145, 0117U000099 , R & D reports Title Synthesis and research of derivatives of fused heterocyclic systems with pyrimidine core popup.stage_title Head Smolii Oleg B., Доктор хімічних наук Registration Date 02-01-2021 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description2 Approaches to the synthesis of new annelated pyrrolo[2,3-d]pyrimidines and functionalized 7-deazapurine derivatives have been developed, which may be promising for further modifications. A number of new functionally substituted pyrrolo[2,3-d]pyrimidine-6-carboxylic acid derivatives were synthesized, the iodination of the obtained compounds was studied, and the dependences of the direction of reactions on the nature of the reagent and the conditions were carried out. It is shown that the products of the iodolactonization reaction are convenient and available reagents in the synthesis of new polycyclic systems with pyrrolo[2,3-d]pyrimidine moiety. The inhibitory activity of 4,7-substituted pyrazino[1', 2':1,5]pyrrolo[2,3-d]pyrimidine derivatives was investigated and compounds showing telomerase inhibitory activity at micromolar concentrations were found. The obtained experimental data on the inhibitory effect together with the results of molecular modeling became the basis for further chemical optimization of the structure of annelated 7-deazapurine derivatives and the development of specific telomerase inhibitors in the development of antitumor agents. Product Description popup.authors Biletsky Igor І. Verves Evgeniy V. Gaevsky Anatoly Р. Zinchenko Hanna M. Kukuyev Maksym О. Kucher Oleksandr V. Muzychka Lyubov V. Yaremchuk Iryna О. popup.nrat_date 2021-01-02 Close