[5-Arylaminouracil 衍生物的细胞毒性研究]。

Q3 Medicine
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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引用次数: 0

摘要

我们之前已经证明,5-芳基氨基脲嘧啶衍生物可以通过各种机制抑制 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 细胞株具有剂量依赖性毒性作用,半数最大抑制浓度(IC50)分别为 9 μ М 和 2.3 μ М。此类化合物的抗肿瘤活性首次得到证实,可作为进一步研究的起点。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Cytotoxicity Studies of 5-Arylaminouracil Derivatives].

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.

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来源期刊
Molekulyarnaya Biologiya
Molekulyarnaya Biologiya Medicine-Medicine (all)
CiteScore
0.70
自引率
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发文量
131
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