{"title":"Design, Synthesis and Antitumor Activity Evaluation of Indole Derivatives Containing Thiadiazole and Urea Motifs","authors":"Guiyun Wu, Nianlin Feng, Yue Zhou, Chengpeng Li, Xue Yang, Zhurui Li, Chenchen Li, Danping Chen, Zhenchao Wang","doi":"10.1002/slct.202500692","DOIUrl":null,"url":null,"abstract":"<p>A series of novel indole derivatives incorporating urea structural fragments and 1,3,4-thiadiazole moieties (<b>E1-25</b>) were designed and synthesized. The antiproliferative activity of these compounds was assessed using methyl thiazolyl tetrazolium (MTT) assay in four human cancer cell lines, human lung adenocarcinoma cells A549 (A549), prostate cancer cells PC-3 (PC-3), human chronic myeloid leukemia cells (K562), human urinary bladder carcinoma cell line (5637). The results revealed that several compounds exhibited antiproliferative activity, with compound <b>E25</b> showing promising activity against K562 cells, with an IC<sub>50</sub> value of 9.42 µM. The mechanism of action of compound <b>E25</b> was further investigated using apoptosis analysis, which provided evidence of its significant ability to induce cell apoptosis.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 19","pages":""},"PeriodicalIF":1.9000,"publicationDate":"2025-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"ChemistrySelect","FirstCategoryId":"92","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/slct.202500692","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
A series of novel indole derivatives incorporating urea structural fragments and 1,3,4-thiadiazole moieties (E1-25) were designed and synthesized. The antiproliferative activity of these compounds was assessed using methyl thiazolyl tetrazolium (MTT) assay in four human cancer cell lines, human lung adenocarcinoma cells A549 (A549), prostate cancer cells PC-3 (PC-3), human chronic myeloid leukemia cells (K562), human urinary bladder carcinoma cell line (5637). The results revealed that several compounds exhibited antiproliferative activity, with compound E25 showing promising activity against K562 cells, with an IC50 value of 9.42 µM. The mechanism of action of compound E25 was further investigated using apoptosis analysis, which provided evidence of its significant ability to induce cell apoptosis.
期刊介绍：
ChemistrySelect is the latest journal from ChemPubSoc Europe and Wiley-VCH. It offers researchers a quality society-owned journal in which to publish their work in all areas of chemistry. Manuscripts are evaluated by active researchers to ensure they add meaningfully to the scientific literature, and those accepted are processed quickly to ensure rapid online publication.
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