{"title":"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。","authors":"Reham A Mohamed-Ezzat, Galal H Elgemeie","doi":"10.1080/15257770.2024.2341406","DOIUrl":null,"url":null,"abstract":"<p><p>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 <i>via</i> a direct approach starting from potassium cyanocarbonimidodithioate, then the corresponding triazine sulfonamide thioglycosides were generated using the peracylated <i>α</i>-d-<i>gluco</i>- and galacto-pyranosyl bromides. Anti-viral evaluation of compounds <i>in vitro</i> against HCoV-229E virus revealed that some compounds possess promising activity. Compounds <b>4a</b>, <b>4b</b>, <b>4d</b>, <b>6d</b> and <b>6e</b> 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 <i>in vitro</i> anti-proliferative effects against NCI 60 cancer cell lines cell lines were also investigated. Compound <b>4a</b>, the most potent compound among the estimated compounds, revealed remarkably lowest cell growth promotion against CNS cancer SNB-75, and renal cancer UO-31.</p>","PeriodicalId":19343,"journal":{"name":"Nucleosides, Nucleotides & Nucleic Acids","volume":null,"pages":null},"PeriodicalIF":1.1000,"publicationDate":"2024-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"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.\",\"authors\":\"Reham A Mohamed-Ezzat, Galal H Elgemeie\",\"doi\":\"10.1080/15257770.2024.2341406\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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 <i>via</i> a direct approach starting from potassium cyanocarbonimidodithioate, then the corresponding triazine sulfonamide thioglycosides were generated using the peracylated <i>α</i>-d-<i>gluco</i>- and galacto-pyranosyl bromides. Anti-viral evaluation of compounds <i>in vitro</i> against HCoV-229E virus revealed that some compounds possess promising activity. Compounds <b>4a</b>, <b>4b</b>, <b>4d</b>, <b>6d</b> and <b>6e</b> 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 <i>in vitro</i> anti-proliferative effects against NCI 60 cancer cell lines cell lines were also investigated. Compound <b>4a</b>, the most potent compound among the estimated compounds, revealed remarkably lowest cell growth promotion against CNS cancer SNB-75, and renal cancer UO-31.</p>\",\"PeriodicalId\":19343,\"journal\":{\"name\":\"Nucleosides, Nucleotides & Nucleic Acids\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.1000,\"publicationDate\":\"2024-05-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Nucleosides, Nucleotides & Nucleic Acids\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://doi.org/10.1080/15257770.2024.2341406\",\"RegionNum\":4,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nucleosides, Nucleotides & Nucleic Acids","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.1080/15257770.2024.2341406","RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
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.
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.
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.