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  3. Научные публикации ученых УрФУ, проиндексированные в SCOPUS и WoS CC
Please use this identifier to cite or link to this item: http://elar.urfu.ru/handle/10995/118061
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dc.contributor.authorLyapustin, D. N.en
dc.contributor.authorKotovskaya, S. K.en
dc.contributor.authorButorin, I. I.en
dc.contributor.authorUlomsky, E. N.en
dc.contributor.authorRusinov, V. L.en
dc.contributor.authorBabkov, D. A.en
dc.contributor.authorPokhlebin, A. A.en
dc.contributor.authorSpasov, A. A.en
dc.contributor.authorMelekhin, V. V.en
dc.contributor.authorTokhtueva, M. D.en
dc.contributor.authorShcheglova, A. V.en
dc.contributor.authorMakeev, O. G.en
dc.date.accessioned2022-10-19T05:21:21Z-
dc.date.available2022-10-19T05:21:21Z-
dc.date.issued2022-
dc.identifier.citationCK2 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.en
dc.identifier.issn14203049-
dc.identifier.otherhttps://www.scopus.com/inward/record.uri?eid=2-s2.0-85136643468&doi=10.3390%2fmolecules27165239&partnerID=40&md5=b33950423081037b0aa048067409bfd9link
dc.identifier.urihttp://elar.urfu.ru/handle/10995/118061-
dc.description.abstractToday, 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.en
dc.description.sponsorshipMinistry of Education and Science of the Russian Federation, Minobrnauka: FEUZ-2020–0058, H687.42B.223/20en
dc.description.sponsorshipThis 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).en
dc.format.mimetypeapplication/pdfen
dc.language.isoenen
dc.publisherMDPIen
dc.rightsinfo:eu-repo/semantics/openAccessen
dc.sourceMoleculesen
dc.subjectANTITUMOR ACTIVITYen
dc.subjectAZOLO[1,5-A]PYRIMIDINESen
dc.subjectCK2 INHIBITIONen
dc.subjectMULTICOMPONENT REACTIONen
dc.subjectNITRO COMPOUNDSen
dc.subjectANTINEOPLASTIC AGENTen
dc.subjectPYRIMIDINE DERIVATIVEen
dc.subjectCELL PROLIFERATIONen
dc.subjectCHEMICAL STRUCTUREen
dc.subjectCHEMISTRYen
dc.subjectDRUG SCREENINGen
dc.subjectGLIOBLASTOMAen
dc.subjectHEK293 CELL LINEen
dc.subjectHUMANen
dc.subjectSTRUCTURE ACTIVITY RELATIONen
dc.subjectTUMOR CELL LINEen
dc.subjectANTINEOPLASTIC AGENTSen
dc.subjectCELL LINE, TUMORen
dc.subjectCELL PROLIFERATIONen
dc.subjectDRUG SCREENING ASSAYS, ANTITUMORen
dc.subjectGLIOBLASTOMAen
dc.subjectHEK293 CELLSen
dc.subjectHUMANSen
dc.subjectMOLECULAR STRUCTUREen
dc.subjectPYRIMIDINESen
dc.subjectSTRUCTURE-ACTIVITY RELATIONSHIPen
dc.titleCK2 Inhibition and Antitumor Activity of 4,7-Dihydro-6-nitroazolo[1,5-a]pyrimidinesen
dc.typeArticleen
dc.typeinfo:eu-repo/semantics/articleen
dc.typeinfo:eu-repo/semantics/publishedVersionen
dc.identifier.doi10.3390/molecules27165239-
dc.identifier.scopus85136643468-
local.contributor.employeeLyapustin, D.N., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federationen
local.contributor.employeeKotovskaya, S.K., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federationen
local.contributor.employeeButorin, I.I., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federationen
local.contributor.employeeUlomsky, E.N., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federationen
local.contributor.employeeRusinov, V.L., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federationen
local.contributor.employeeBabkov, D.A., Department of Pharmacology Bioinformatics, Scientific Center for Innovative Drugs, Volgograd State Medical University, Volgograd, 400131, Russian Federationen
local.contributor.employeePokhlebin, A.A., Department of Pharmacology Bioinformatics, Scientific Center for Innovative Drugs, Volgograd State Medical University, Volgograd, 400131, Russian Federationen
local.contributor.employeeSpasov, A.A., Department of Pharmacology Bioinformatics, Scientific Center for Innovative Drugs, Volgograd State Medical University, Volgograd, 400131, Russian Federationen
local.contributor.employeeMelekhin, V.V., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federation, Department of Biology, Ural State Medical University, Repina 3, Yekaterinburg, 620014, Russian Federationen
local.contributor.employeeTokhtueva, M.D., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federationen
local.contributor.employeeShcheglova, A.V., Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federation, Department of Biology, Ural State Medical University, Repina 3, Yekaterinburg, 620014, Russian Federationen
local.contributor.employeeMakeev, O.G., Department of Biology, Ural State Medical University, Repina 3, Yekaterinburg, 620014, Russian Federationen
local.issue16-
local.volume27-
dc.identifier.wos000845381100001-
local.contributor.departmentDepartment of Organic and Biomolecular Chemistry, Ural Federal University, Mira St. 19, Ekaterinburg, 620002, Russian Federationen
local.contributor.departmentDepartment of Pharmacology Bioinformatics, Scientific Center for Innovative Drugs, Volgograd State Medical University, Volgograd, 400131, Russian Federationen
local.contributor.departmentDepartment of Biology, Ural State Medical University, Repina 3, Yekaterinburg, 620014, Russian Federationen
local.identifier.pure30849918-
local.description.order5239-
local.identifier.eid2-s2.0-85136643468-
local.identifier.wosWOS:000845381100001-
local.fund.feuzFEUZ-2020-0058-
local.identifier.pmid36014483-
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