Debashish Tomar, Axel Steinbrueck, Adam C. Sedgwick, Matthew S. Levine, Jonathan L. Sessler and Nils Metzler-Nolte
{"title":"糖苷酶激活的细胞毒性铁螯合剂用于靶向癌症治疗的前药。","authors":"Debashish Tomar, Axel Steinbrueck, Adam C. Sedgwick, Matthew S. Levine, Jonathan L. Sessler and Nils Metzler-Nolte","doi":"10.1039/D5MD00232J","DOIUrl":null,"url":null,"abstract":"<p >New glycoside-prodrugs based on the iron chelator deferasirox were designed. Selective enzymatic activation by glycosidases was observed within 24 hours, accompanied by cancer cell-selective cytotoxicity. Notably, derivative <strong>3a</strong>, bearing a β-<small>D</small>-galactose moiety, showed promising selective activity against galactosidase overexpressing OvCar-3 cells (IC<small><sub>50</sub></small> 9.1 ± 1.6 μM) while maintaining low activity against fibroblast control GM5756 cells (IC<small><sub>50</sub></small> > 100 μM).</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":" 8","pages":" 3507-3511"},"PeriodicalIF":3.6000,"publicationDate":"2025-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12177571/pdf/","citationCount":"0","resultStr":"{\"title\":\"Glycosidase-activated prodrugs of a cytotoxic iron chelator for targeted cancer therapy†\",\"authors\":\"Debashish Tomar, Axel Steinbrueck, Adam C. Sedgwick, Matthew S. Levine, Jonathan L. Sessler and Nils Metzler-Nolte\",\"doi\":\"10.1039/D5MD00232J\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >New glycoside-prodrugs based on the iron chelator deferasirox were designed. Selective enzymatic activation by glycosidases was observed within 24 hours, accompanied by cancer cell-selective cytotoxicity. Notably, derivative <strong>3a</strong>, bearing a β-<small>D</small>-galactose moiety, showed promising selective activity against galactosidase overexpressing OvCar-3 cells (IC<small><sub>50</sub></small> 9.1 ± 1.6 μM) while maintaining low activity against fibroblast control GM5756 cells (IC<small><sub>50</sub></small> > 100 μM).</p>\",\"PeriodicalId\":21462,\"journal\":{\"name\":\"RSC medicinal chemistry\",\"volume\":\" 8\",\"pages\":\" 3507-3511\"},\"PeriodicalIF\":3.6000,\"publicationDate\":\"2025-06-19\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12177571/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"RSC medicinal chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://pubs.rsc.org/en/content/articlelanding/2025/md/d5md00232j\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"RSC medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://pubs.rsc.org/en/content/articlelanding/2025/md/d5md00232j","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Glycosidase-activated prodrugs of a cytotoxic iron chelator for targeted cancer therapy†
New glycoside-prodrugs based on the iron chelator deferasirox were designed. Selective enzymatic activation by glycosidases was observed within 24 hours, accompanied by cancer cell-selective cytotoxicity. Notably, derivative 3a, bearing a β-D-galactose moiety, showed promising selective activity against galactosidase overexpressing OvCar-3 cells (IC50 9.1 ± 1.6 μM) while maintaining low activity against fibroblast control GM5756 cells (IC50 > 100 μM).
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
