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Vol 58(2024) N 2 p. 328-335; DOI 10.1134/S0026893324020079 Full Text

V.A. Kezin1, E.S. Matyugina1, S.A. Surzhikov1, M.S. Novikov2, A.A. Maslova1, I.L. Karpenko1, A.V. Ivanov1, S.N. Kochetkov1, A.L. Khandazhinskaya1*

Cytotoxicity Studies of 5-Arylaminouracil Derivatives

1Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, 119991 Russia
2Volgograd State Medical University, Volgograd, 400131 Russia


*khandazhinskaya@bk.ru
Received - 2023-09-14; Revised - 2023-10-13; Accepted - 2023-10-13

We have previously shown that 5-arylaminouracil derivatives can inhibit HIV-1, herpesviruses, mycobacteria, and other pathogens through various mechanisms. The purpose of this study was to evaluate the potential of 5-arylaminouracils and their derivatives against leukemia, neuroblastoma, and glial brain tumors. 5-Aminouracils with various substituents and their 5'-norcabocyclic and ribo derivatives were screened for cytotoxicity against two neuroblastoma cell lines (SH-SY5Y and IMR-32), K-562 lymphoblastic cells, HL-60 promyeoloblastic cells, and low-passage variants of well-differentiated glioblastoma multiforme (GBM5522 and GBM6138). Cytotoxicity assessment by the standard MTT test showed that most of the compounds lack significant toxicity towards the above cells. However, 5-(4-isopropylphenylamine)uracil and 5-(4-tert-butylphenylamine)uracil exhibited a dose-dependent toxic effect towards the GBM6138 cell line with half-maximal inhibitory concentrations (IC50) of 9 and 2.3 μМ, respectively. Antitumor activity was for the first time demonstrated for compounds of this type and can serve as a starting point for further research.

uracil derivatives, synthesis, antitumor activity, leukemia, glioma, neuroblastoma



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