{"title":"Modular Synthesis of Bioactive Selenoheterocycles for Efficient Cancer Therapy via Electrochemical Selenylation/Cyclization","authors":"Wenyan Xu, Chengwei Zheng, Mu Chen, Xin Deng, Lingmin Zhang, Xueping Lei, Lu Liang, Xiyong Yu, Xinwei Hu, Juyun He, Shuimu Lin, Zhixiong Ruan","doi":"10.1021/acs.jmedchem.4c02724","DOIUrl":null,"url":null,"abstract":"A green, efficient, and environmentally friendly electrochemical strategy was developed for synthesizing a series of selenoheterocyclic compounds. The antitumor activities of these compounds were evaluated, revealing that compounds <b>4o</b>, <b>5n</b>, and <b>5o</b> demonstrated remarkable antitumor efficacy. These compounds effectively inhibited lung cancer by inducing cell apoptosis, causing DNA damage, and suppressing the progression of epithelial–mesenchymal transition. Notably, compound <b>5o</b> was identified as the first inhibitor of DEAD-box helicase 10 (DDX10). An <i>in vivo</i> xenograft assay further confirmed the therapeutic potential of compound <b>5o</b>, demonstrating tumor growth inhibition rates of 60%, 78%, and 88% at doses of 5 mg/kg, 10 mg/kg, and 20 mg/kg, respectively. This study highlights a promising chemotherapeutic agent for the effective treatment of lung cancer.","PeriodicalId":46,"journal":{"name":"Journal of Medicinal Chemistry","volume":"13 1","pages":""},"PeriodicalIF":6.8000,"publicationDate":"2025-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acs.jmedchem.4c02724","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
A green, efficient, and environmentally friendly electrochemical strategy was developed for synthesizing a series of selenoheterocyclic compounds. The antitumor activities of these compounds were evaluated, revealing that compounds 4o, 5n, and 5o demonstrated remarkable antitumor efficacy. These compounds effectively inhibited lung cancer by inducing cell apoptosis, causing DNA damage, and suppressing the progression of epithelial–mesenchymal transition. Notably, compound 5o was identified as the first inhibitor of DEAD-box helicase 10 (DDX10). An in vivo xenograft assay further confirmed the therapeutic potential of compound 5o, demonstrating tumor growth inhibition rates of 60%, 78%, and 88% at doses of 5 mg/kg, 10 mg/kg, and 20 mg/kg, respectively. This study highlights a promising chemotherapeutic agent for the effective treatment of lung cancer.
期刊介绍:
The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents.
The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.