Please use this identifier to cite or link to this item: http://hdl.handle.net/10995/118061
Title: CK2 Inhibition and Antitumor Activity of 4,7-Dihydro-6-nitroazolo[1,5-a]pyrimidines
Authors: 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.
Issue Date: 2022
Publisher: MDPI
Citation: 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.
Abstract: 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.
Keywords: 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://hdl.handle.net/10995/118061
Access: info:eu-repo/semantics/openAccess
SCOPUS ID: 85136643468
ISSN: 14203049
DOI: 10.3390/molecules27165239
metadata.dc.description.sponsorship: 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).
Appears in Collections:Научные публикации, проиндексированные в SCOPUS и WoS CC

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