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http://elar.urfu.ru/handle/10995/118061
Название: | CK2 Inhibition and Antitumor Activity of 4,7-Dihydro-6-nitroazolo[1,5-a]pyrimidines |
Авторы: | Lyapustin, D. N. Kotovskaya, S. K. Butorin, I. I. Ulomsky, E. N. Rusinov, V. L. Babkov, D. A. Pokhlebin, A. A. Spasov, A. A. Melekhin, V. V. Tokhtueva, M. D. Shcheglova, A. V. Makeev, O. G. |
Дата публикации: | 2022 |
Издатель: | MDPI |
Библиографическое описание: | CK2 Inhibition and Antitumor Activity of 4,7-Dihydro-6-nitroazolo[1,5-a]pyrimidines / D. N. Lyapustin, S. K. Kotovskaya, I. I. Butorin et al. // Molecules. — 2022. — Vol. 27. — Iss. 16. — 5239. |
Аннотация: | Today, cancer is one of the most widespread and dangerous human diseases with a high mortality rate. Nevertheless, the search and application of new low-toxic and effective drugs, combined with the timely diagnosis of diseases, makes it possible to cure most types of tumors at an early stage. In this work, the range of new polysubstituted 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines was extended. The structure of all the obtained compounds was confirmed by the data of 1H, 13C NMR spectroscopy, IR spectroscopy, and elemental analysis. These compounds were evaluated against human recombinant CK2 using the ADP-GloTM assay. In addition, the IC50 parameters were calculated based on the results of the MTT test against glioblastoma (A-172), embryonic rhabdomyosarcoma (Rd), osteosarcoma (Hos), and human embryonic kidney (Hek-293) cells. Compounds 5f, 5h, and 5k showed a CK2 inhibitory activity close to the reference molecule (staurosporine). The most potential compound in the MTT test was 5m with an IC50 from 13 to 27 µM. Thus, our results demonstrate that 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines are promising for further investigation of their antitumor properties. © 2022 by the authors. |
Ключевые слова: | ANTITUMOR ACTIVITY AZOLO[1,5-A]PYRIMIDINES CK2 INHIBITION MULTICOMPONENT REACTION NITRO COMPOUNDS ANTINEOPLASTIC AGENT PYRIMIDINE DERIVATIVE CELL PROLIFERATION CHEMICAL STRUCTURE CHEMISTRY DRUG SCREENING GLIOBLASTOMA HEK293 CELL LINE HUMAN STRUCTURE ACTIVITY RELATION TUMOR CELL LINE ANTINEOPLASTIC AGENTS CELL LINE, TUMOR CELL PROLIFERATION DRUG SCREENING ASSAYS, ANTITUMOR GLIOBLASTOMA HEK293 CELLS HUMANS MOLECULAR STRUCTURE PYRIMIDINES STRUCTURE-ACTIVITY RELATIONSHIP |
URI: | http://elar.urfu.ru/handle/10995/118061 |
Условия доступа: | info:eu-repo/semantics/openAccess |
Идентификатор SCOPUS: | 85136643468 |
Идентификатор WOS: | 000845381100001 |
Идентификатор PURE: | 30849918 |
ISSN: | 14203049 |
DOI: | 10.3390/molecules27165239 |
Сведения о поддержке: | Ministry of Education and Science of the Russian Federation, Minobrnauka: FEUZ-2020–0058, H687.42B.223/20 This work was financially supported by the Ministry of Science and Higher Education of the Russian Federation, State Contract № FEUZ-2020–0058 (H687.42B.223/20). |
Располагается в коллекциях: | Научные публикации ученых УрФУ, проиндексированные в SCOPUS и WoS CC |
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Файл | Описание | Размер | Формат | |
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2-s2.0-85136643468.pdf | 1,43 MB | Adobe PDF | Просмотреть/Открыть |
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