Novel synthesis of the first new class of triazine sulfonamide thioglycosides and the evaluation of their anti-tumor and anti-viral activities against human coronavirus.

IF 1.1 4区 生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Reham A Mohamed-Ezzat, Galal H Elgemeie
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引用次数: 0

Abstract

Novel class of triazine sulfonamide thioglycosides was designed and synthesized. Those novel structures comprising three essential and pharmacological significant moieties such as the triazine, sulfonamide, and thioglycosidic scaffolds. The triazine sulfonamides were furnished via a direct approach starting from potassium cyanocarbonimidodithioate, then the corresponding triazine sulfonamide thioglycosides were generated using the peracylated α-d-gluco- and galacto-pyranosyl bromides. Anti-viral evaluation of compounds in vitro against HCoV-229E virus revealed that some compounds possess promising activity. Compounds 4a, 4b, 4d, 6d and 6e indicate from moderate to low antiviral activity against low pathogenic coronavirus 229E in comparison with remdesivir at a concentration of 100 µg/mL. Additionally their in vitro anti-proliferative effects against NCI 60 cancer cell lines cell lines were also investigated. Compound 4a, the most potent compound among the estimated compounds, revealed remarkably lowest cell growth promotion against CNS cancer SNB-75, and renal cancer UO-31.

第一类新型三嗪磺酰胺硫代糖苷的新合成及其对人类冠状病毒的抗肿瘤和抗病毒活性评估。
设计并合成了新型三嗪磺酰胺硫代糖苷类化合物。这些新型结构包括三个重要的药理学分子,如三嗪、磺酰胺和硫代糖苷支架。三嗪磺酰胺是以二硫代氰基碳亚氨基钾为起点通过直接方法合成的,然后利用过酰基化的α-d-葡糖基和半乳糖基溴化物生成相应的三嗪磺酰胺硫代糖苷。化合物在体外对 HCoV-229E 病毒的抗病毒评估显示,一些化合物具有良好的活性。与浓度为 100 µg/mL 的雷米替韦相比,化合物 4a、4b、4d、6d 和 6e 对低致病性冠状病毒 229E 的抗病毒活性从中等到较低不等。此外,还研究了它们对 NCI 60 癌细胞株的体外抗增殖作用。化合物 4a 是估计化合物中最有效的化合物,它对中枢神经系统癌症 SNB-75 和肾癌 UO-31 的细胞生长促进作用明显降低。
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来源期刊
Nucleosides, Nucleotides & Nucleic Acids
Nucleosides, Nucleotides & Nucleic Acids 生物-生化与分子生物学
CiteScore
2.60
自引率
7.70%
发文量
91
审稿时长
6 months
期刊介绍: Nucleosides, Nucleotides & Nucleic Acids publishes research articles, short notices, and concise, critical reviews of related topics that focus on the chemistry and biology of nucleosides, nucleotides, and nucleic acids. Complete with experimental details, this all-inclusive journal emphasizes the synthesis, biological activities, new and improved synthetic methods, and significant observations related to new compounds.
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