Kseniya S. Kovaleva, Olga I. Yarovaya, Irina A. Chernyshova, Alexandra L. Zakharenko, Sergey V. Cheresiz, Amirhossein Azimirad, Andrey G. Pokrovsky, Olga I. Lavrik, Nariman F. Salakhutdinov
{"title":"Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1","authors":"Kseniya S. Kovaleva, Olga I. Yarovaya, Irina A. Chernyshova, Alexandra L. Zakharenko, Sergey V. Cheresiz, Amirhossein Azimirad, Andrey G. Pokrovsky, Olga I. Lavrik, Nariman F. Salakhutdinov","doi":"10.3390/m1743","DOIUrl":null,"url":null,"abstract":"New imidazolidine-2,4,5-triones with norabietic, nordehydroabietic, and adamantane substituents were synthesized by reacting oxalyl chloride and the corresponding ureas, providing good yields. Bioisosteric replacement of the ureide group with a parabanic acid fragment made it possible to increase the solubility of compounds and conduct biological studies. The compounds inhibit the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 in submicromolar concentrations. Cytotoxic concentrations were also studied on the glioblastoma cell line SNB19.","PeriodicalId":18761,"journal":{"name":"Molbank","volume":" 38","pages":"0"},"PeriodicalIF":0.6000,"publicationDate":"2023-11-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molbank","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3390/m1743","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
引用次数: 0
Abstract
New imidazolidine-2,4,5-triones with norabietic, nordehydroabietic, and adamantane substituents were synthesized by reacting oxalyl chloride and the corresponding ureas, providing good yields. Bioisosteric replacement of the ureide group with a parabanic acid fragment made it possible to increase the solubility of compounds and conduct biological studies. The compounds inhibit the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 in submicromolar concentrations. Cytotoxic concentrations were also studied on the glioblastoma cell line SNB19.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
