Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′- fluorothymidine (FLT) pro-nucleotides

VelanguparackelW.; HamonN.; BalzariniJ.; McGuiganC.; WestwellA.D.

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Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′- fluorothymidine (FLT) pro-nucleotides

机译：3'-脱氧-3'-氟脲酰胺（FLT）核苷酸的合成，抗HIV和细胞抑制评价

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摘要

A series of pro-nucleotide phosphoramidates and phosphorodiamidates of the antiviral lead compound 3′-deoxy-3′-fluorothymidine (FLT) have been designed and synthesized. In vitro antiretroviral and cytostatic studies revealed potent (sub-micromolar) inhibition of HIV-1 and HIV-2 replication, with retention of activity in thymidine kinase-negative cell models, as predicted by the ProTide concept.

机译：已经设计和合成了一系列灭毒铅化合物3'-脱氧-3'-氟脱水线（FLT）的磷酰胺磷酰胺和磷酸二胺基化物。体外抗逆转录病毒和细胞抑制研究显示了HIV-1和HIV-2复制的有效（亚微摩尔）抑制，并保留了胸苷激酶阴性细胞模型中的活性，如受特定概念所预测的。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2014年第10期|共4页
作者
VelanguparackelW.; HamonN.; BalzariniJ.; McGuiganC.; WestwellA.D.;
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作者单位

School of Pharmacy and Pharmaceutical Sciences Cardiff University Redwood Building King Edward;

School of Pharmacy and Pharmaceutical Sciences Cardiff University Redwood Building King Edward;

Rega Institute for Medical Research KU Leuven Minderbroedersstraat 10 B-3000 Leuven Belgium;

School of Pharmacy and Pharmaceutical Sciences Cardiff University Redwood Building King Edward;

School of Pharmacy and Pharmaceutical Sciences Cardiff University Redwood Building King Edward;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Anticancer; Antiviral; Nucleosides; Phosphoramidates; Pro-drugs; Pro-nucleotides;

机译：抗癌;抗病毒;核苷;磷酰胺化;pro-mails;pro-核苷酸;

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专利

1. Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′- fluorothymidine (FLT) pro-nucleotides [J] . VelanguparackelW., HamonN., BalzariniJ., Bioorganic and Medicinal Chemistry Letters . 2014,第10期

机译：3'-脱氧-3'-氟脲酰胺（FLT）核苷酸的合成，抗HIV和细胞抑制评价
2. Evaluation of the radiochemical impurities arising during the competitive fluorination of nosyl group during the synthesis of 3′-deoxy-3′- fluorothymidine, [~(18)F]FLT [J] . Nandy S.K., Krishnamurthy N.V., Rajan M.G.R. Journal of Radioanalytical and Nuclear Chemistry: An International Journal Dealing with All Aspects and Applications of Nuclear Chemistry . 2010,第1期

机译：评价3'-脱氧-3'-氟胸苷[[（（18）F] FLT）合成过程中壬基竞争性氟化过程中产生的放射性化学杂质
3. Evaluation of the radiochemical impurities arising during the competitive fluorination of nosyl group during the synthesis of 3′-deoxy-3′-fluorothymidine, [18F]FLT [J] . S. K. Nandy, N. V. Krishnamurthy, M. G. R. Rajan Journal of Radioanalytical and Nuclear Chemistry . 2010,第1期

机译：3'-脱氧-3'-氟胸苷[[sup> 18 F] FLT的合成过程中，在壬基的竞争性氟化过程中产生的放射性化学杂质的评价
4. Methotrexate Containing Oligopeptide Conjugates: Synthesis and in vitro Cytostatic Effect [C] . Zoltan Banoczi, Marton Florian, Erika Orban American Peptide Symposium . 2013

机译：含有寡肽缀合物的甲氨蝶呤：合成和体外细胞抑制效果
5. Characterization of transport of positron emission tomography tracer 3'-deoxy-3'-fluorothymidine by nucleoside transporters. [D] . Paproski, Robert Joseph. 2010

机译：正电子发射断层扫描示踪剂3'-脱氧-3'-氟胸苷通过核苷转运蛋白的转运特征。
6. Exploratory Analysis of 18F-3’-deoxy-3’-fluorothymidine (18F-FLT) PET/CT-Based Radiomics for the Early Evaluation of Response to Neoadjuvant Chemotherapy in Patients With Locally Advanced Breast Cancer [O] . Lorenzo Fantini, Maria Luisa Belli, Irene Azzali, 2021

机译：18F-3-脱氧-3-氟脲酰胺（18F-FLT）PET / CT基辐射瘤的探索性分析早期评估局部晚期乳腺癌患者对新辅助化疗的早期评价
7. Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′-fluorothymidine (FLT) pro-nucleotides [O] . Velanguparackel, Winnie, Hamon, Nadege, Balzarini, Jan, 2014

机译：3'-脱氧-3'-氟胸苷（FLT）前核苷酸的合成，抗HIV和细胞抑制作用评估

Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′- fluorothymidine (FLT) pro-nucleotides

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