• 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

2'-氟修饰的核苷膦酸酯的合成及其抗HIV活性:GS-9148类似物

Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148.

作者信息

Mackman Richard L, Lin Kuei-Ying, Boojamra Constantine G, Hui Hon, Douglas Janet, Grant Deborah, Petrakovsky Oleg, Prasad Vidya, Ray Adrian S, Cihlar Tomas

机构信息

Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.

出版信息

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1116-9. doi: 10.1016/j.bmcl.2007.11.126. Epub 2007 Dec 5.

DOI:10.1016/j.bmcl.2007.11.126
PMID:18082402
Abstract

Modified purine analogs of GS-9148 [5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yloxymethyl]-phosphonic acid (2'-Fd4AP) were synthesized and their anti-HIV potency evaluated. The antiviral activity of guanosine analog (2'-Fd4GP) was comparable that of to 2'-Fd4AP in MT-2 cells, but selectivity was reduced.

摘要

合成了GS-9148 [5-(6-氨基嘌呤-9-基)-4-氟-2,5-二氢呋喃-2-基氧甲基]-膦酸(2'-Fd4AP)的修饰嘌呤类似物,并评估了它们的抗HIV效力。鸟苷类似物(2'-Fd4GP)在MT-2细胞中的抗病毒活性与2'-Fd4AP相当,但选择性降低。

相似文献

1
Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148.2'-氟修饰的核苷膦酸酯的合成及其抗HIV活性:GS-9148类似物
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1116-9. doi: 10.1016/j.bmcl.2007.11.126. Epub 2007 Dec 5.
2
Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.新型核苷膦酸类HIV逆转录酶抑制剂GS-9148(2'-氟-2'-脱氧腺苷磷酸酯)的合成及其抗HIV活性
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1120-3. doi: 10.1016/j.bmcl.2007.11.125. Epub 2007 Dec 5.
3
Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates.核糖修饰的核苷膦酸酯的合成、抗HIV活性及耐药性研究
Bioorg Med Chem Lett. 2007 Dec 15;17(24):6785-9. doi: 10.1016/j.bmcl.2007.10.038. Epub 2007 Oct 17.
4
Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.GS-9131 的发现:新型核苷膦酸 HIV 逆转录酶(RT)抑制剂 GS-9148 的酰胺前药的设计、合成与优化。
Bioorg Med Chem. 2010 May 15;18(10):3606-17. doi: 10.1016/j.bmc.2010.03.041. Epub 2010 Mar 27.
5
Design and synthesis of α-carboxy nucleoside phosphonate analogues and evaluation as HIV-1 reverse transcriptase-targeting agents.α-羧基核苷膦酸酯类似物的设计与合成及其作为HIV-1逆转录酶靶向剂的评价
J Org Chem. 2015 Mar 6;80(5):2479-93. doi: 10.1021/jo502549y. Epub 2015 Jan 9.
6
Synthesis of 3'-halo-5'-norcarbocyclic nucleoside phosphonates as potent anti-HIV agents.作为强效抗艾滋病毒药物的3'-卤代-5'-去碳环核苷膦酸酯的合成。
Eur J Med Chem. 2018 Apr 25;150:642-654. doi: 10.1016/j.ejmech.2018.03.038. Epub 2018 Mar 14.
7
Exploring the role of the α-carboxyphosphonate moiety in the HIV-RT activity of α-carboxy nucleoside phosphonates.探索α-羧基膦酸酯部分在α-羧基核苷膦酸酯的HIV逆转录酶活性中的作用。
Org Biomol Chem. 2016 Feb 28;14(8):2454-65. doi: 10.1039/c5ob02507a.
8
Membrane Permeable, Bioreversibly Modified Prodrugs of Nucleoside Diphosphate-γ-Phosphonates.膜通透性、核苷二磷酸-γ-膦酸酯的生物可逆修饰前药。
J Med Chem. 2020 Oct 22;63(20):11990-12007. doi: 10.1021/acs.jmedchem.0c01294. Epub 2020 Oct 14.
9
Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131.GS-9148的设计与特性分析,GS-9148是一种对1型人类免疫缺陷病毒核苷抗性变体有活性的新型核苷酸类似物,以及其口服生物可利用的膦酸酰胺前药GS-9131。
Antimicrob Agents Chemother. 2008 Feb;52(2):655-65. doi: 10.1128/AAC.01215-07. Epub 2007 Dec 3.
10
Synthesis and antiretroviral activity of novel 4'-fluoro-5'-deoxyphosphonic acid carbocyclic nucleoside analogs.新型4'-氟-5'-脱氧膦酸碳环核苷类似物的合成及其抗逆转录病毒活性
Nucleosides Nucleotides Nucleic Acids. 2014;33(10):678-95. doi: 10.1080/15257770.2014.920506.

引用本文的文献

1
Adenine: an important drug scaffold for the design of antiviral agents.腺嘌呤:用于设计抗病毒药物的重要药物骨架。
Acta Pharm Sin B. 2015 Sep;5(5):431-41. doi: 10.1016/j.apsb.2015.07.002. Epub 2015 Sep 2.