• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

5-（三氟甲基）-和5-（五氟乙基）嘧啶核苷类似物的合成与生物活性

Synthesis and biological activity of 5-(trifluoromethyl)- and 5-(pentafluoroethyl)pyrimidine nucleoside analogues.

作者信息

Lin T S, Gao Y S

出版信息

J Med Chem. 1983 Apr;26(4):598-601. doi: 10.1021/jm00358a028.

DOI:10.1021/jm00358a028
PMID:6300402
Abstract

Various 5-substituted perfluoroalkylpyrimidine nucleoside analogues have been synthesized, and their biological activity against L1210, S-180, Vero cells, and herpes simplex virus type 1 (HSV-1) was evaluated. The 5-trifluoromethyl derivatives, 7 and 9, showed significant antiviral activity against HSV-1 with ED50 values of 7 and 5 microM, respectively. In addition, the unblocked nucleoside 9 was found to be about 64-fold less toxic to the host Vero cells and gave a favorable therapeutic index of 64 against HSV-1 in vitro.

摘要

已合成了多种5-取代的全氟烷基嘧啶核苷类似物，并评估了它们对L1210、S-180、Vero细胞和1型单纯疱疹病毒（HSV-1）的生物活性。5-三氟甲基衍生物7和9对HSV-1显示出显著的抗病毒活性，ED50值分别为7和5微摩尔。此外，发现未封闭的核苷9对宿主Vero细胞的毒性约低64倍，并且在体外对HSV-1的治疗指数为64，效果良好。

相似文献

1
Synthesis and biological activity of 5-(trifluoromethyl)- and 5-(pentafluoroethyl)pyrimidine nucleoside analogues.5-（三氟甲基）-和5-（五氟乙基）嘧啶核苷类似物的合成与生物活性
J Med Chem. 1983 Apr;26(4):598-601. doi: 10.1021/jm00358a028.
2
Nucleic acid related compounds. 47. Synthesis and biological activities of pyrimidine and purine "acyclic" nucleoside analogues.核酸相关化合物。47. 嘧啶和嘌呤“无环”核苷类似物的合成及生物活性
J Med Chem. 1984 Nov;27(11):1486-92. doi: 10.1021/jm00377a018.
3
Synthesis and anti-herpes virus activity of 2'-deoxy-4'-thiopyrimidine nucleosides.2'-脱氧-4'-硫代嘧啶核苷的合成及其抗疱疹病毒活性
J Med Chem. 1996 Feb 2;39(3):789-95. doi: 10.1021/jm950029r.
4
Synthesis and anticancer activity of various 3'-deoxy pyrimidine nucleoside analogues and crystal structure of 1-(3-deoxy-beta-D-threo-pentofuranosyl)cytosine.多种3'-脱氧嘧啶核苷类似物的合成与抗癌活性以及1-(3-脱氧-β-D-苏式-戊呋喃糖基)胞嘧啶的晶体结构
J Med Chem. 1991 Feb;34(2):693-701. doi: 10.1021/jm00106a034.
5
Arabinofuranosylpyrrolo[2,3-d]pyrimidines as potential agents for human cytomegalovirus infections.阿拉伯呋喃糖基吡咯并[2,3-d]嘧啶作为人类巨细胞病毒感染的潜在药物。
J Med Chem. 1990 Dec;33(12):3160-9. doi: 10.1021/jm00174a011.
6
Synthesis and biological activities of some uronic acids, uronates, uronamides, and urononitriles of pyrimidine nucleosides.一些嘧啶核苷的糖醛酸、糖醛酸盐、糖酰胺和糖腈的合成及生物活性
J Med Chem. 1978 Nov;21(11):1141-6. doi: 10.1021/jm00209a010.
7
Synthesis and biological evaluation of 2',3'-dideoxy-L-pyrimidine nucleosides as potential antiviral agents against human immunodeficiency virus (HIV) and hepatitis B virus (HBV).2',3'-二脱氧-L-嘧啶核苷作为抗人类免疫缺陷病毒（HIV）和乙型肝炎病毒（HBV）潜在抗病毒药物的合成及生物学评价
J Med Chem. 1994 Mar 18;37(6):798-803. doi: 10.1021/jm00032a013.
8
Selective in vitro and in vivo activities of 5-(2-haloalkyl)pyrimidine nucleoside analogs, particularly 5-(2-chloroethyl)-2'-deoxyuridine, against herpes simplex virus.5-(2-卤代烷基)嘧啶核苷类似物，特别是5-(2-氯乙基)-2'-脱氧尿苷对单纯疱疹病毒的体外和体内选择性活性。
Antimicrob Agents Chemother. 1985 Aug;28(2):246-51. doi: 10.1128/AAC.28.2.246.
9
Synthesis and biological activity of 5-phenylselenenyl-substituted pyrimidine nucleosides.5-苯基硒代取代嘧啶核苷的合成与生物活性
J Med Chem. 1986 Jul;29(7):1293-5. doi: 10.1021/jm00157a031.
10
Synthesis and antineoplastic activity of a novel series of phosphoramide mustard analogues of pyrimidine deoxyribonucleosides.
J Med Chem. 1980 Nov;23(11):1235-7. doi: 10.1021/jm00185a018.