Synthesis, anti-HIV activity and stability studies of 3'-azido-2',3'-dideoxythymidine 5'-fluorophosphate.

D Egron, A A Arzumanov, N B Dyatkina, A Krayevsky, J L Imbach, A M Aubertin, G Gosselin, C Périgaud
{"title":"Synthesis, anti-HIV activity and stability studies of 3'-azido-2',3'-dideoxythymidine 5'-fluorophosphate.","authors":"D Egron,&nbsp;A A Arzumanov,&nbsp;N B Dyatkina,&nbsp;A Krayevsky,&nbsp;J L Imbach,&nbsp;A M Aubertin,&nbsp;G Gosselin,&nbsp;C Périgaud","doi":"10.1080/15257779908041621","DOIUrl":null,"url":null,"abstract":"<p><p>The synthesis, in vitro anti-HIV activity, and stability studies of AZT 5'-fluorophosphate (F-AZTMP) are reported. The present results demonstrate that such compound is a bioprecursor of its parent 5'-mononucleotide (AZTMP) but its biotransformation does not allow its selective intracellular delivery. Moreover, several attempts were carried out in order to improve the biological activity of this compound by the use of a SATE prodrug strategy.</p>","PeriodicalId":19222,"journal":{"name":"Nucleosides & nucleotides","volume":"18 4-5","pages":"983-4"},"PeriodicalIF":0.0000,"publicationDate":"1999-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/15257779908041621","citationCount":"4","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nucleosides & nucleotides","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/15257779908041621","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 4

Abstract

The synthesis, in vitro anti-HIV activity, and stability studies of AZT 5'-fluorophosphate (F-AZTMP) are reported. The present results demonstrate that such compound is a bioprecursor of its parent 5'-mononucleotide (AZTMP) but its biotransformation does not allow its selective intracellular delivery. Moreover, several attempts were carried out in order to improve the biological activity of this compound by the use of a SATE prodrug strategy.

3'-叠氮-2',3'-二脱氧胸腺嘧啶5'-氟磷酸盐的合成、抗hiv活性及稳定性研究。
本文报道了azt5′-氟磷酸盐(F-AZTMP)的合成、体外抗hiv活性和稳定性研究。目前的研究结果表明,该化合物是其亲本5'-单核苷酸(AZTMP)的生物递质,但其生物转化不允许其选择性细胞内递送。此外,为了提高该化合物的生物活性,进行了几次尝试,以使用SATE药前策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信