Cytotoxicity Studies of 5-Arylaminouracil Derivatives

IF 1.5 4区生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Molecular Biology Pub Date : 2024-04-09 DOI:10.1134/s0026893324020079

V. A. Kezin, E. S. Matyugina, S. A. Surzhikov, M. S. Novikov, A. A. Maslova, I. L. Karpenko, A. V. Ivanov, S. N. Kochetkov, A. L. Khandazhinskaya

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Abstract

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 μM, respectively. Antitumor activity was for the first time demonstrated for compounds of this type and can serve as a starting point for further research.

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5-Arylaminouracil 衍生物的细胞毒性研究

摘要我们曾研究表明，5-芳基氨基脲嘧啶衍生物可通过各种机制抑制 HIV-1、疱疹病毒、分枝杆菌和其他病原体。本研究的目的是评估 5-芳基氨基脲嘧啶及其衍生物对白血病、神经母细胞瘤和脑胶质瘤的潜在作用。研究人员筛选了具有不同取代基的 5-氨基脲嘧啶及其 5'-norcabocyclic 和 ribo 衍生物对两种神经母细胞瘤细胞系（SH-SY5Y 和 IMR-32）、K-562 淋巴母细胞、HL-60 原叶母细胞和低分化胶质母细胞瘤多形性变体（GBM5522 和 GBM6138）的细胞毒性。通过标准的 MTT 试验进行的细胞毒性评估表明，大多数化合物对上述细胞都没有明显的毒性。然而，5-(4-异丙基苯胺)脲嘧啶和 5-(4-叔丁基苯胺)脲嘧啶对 GBM6138 细胞系具有剂量依赖性毒性作用，半数最大抑制浓度（IC50）分别为 9 和 2.3 μM。这是此类化合物首次显示出抗肿瘤活性，可作为进一步研究的起点。

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来源期刊

Molecular Biology 生物-生化与分子生物学

CiteScore

1.30

自引率

8.30%

发文量

审稿时长

3 months

期刊介绍： Molecular Biology is an international peer reviewed journal that covers a wide scope of problems in molecular, cell and computational biology including genomics, proteomics, bioinformatics, molecular virology and immunology, molecular development biology, molecular evolution and related areals. Molecular Biology publishes reviews, experimental and theoretical works. Every year, the journal publishes special issues devoted to most rapidly developing branches of physical-chemical biology and to the most outstanding scientists.