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强效选择性抗HIV药物——2',3'-二脱氧-3'-氟-2-硫代胸苷（S2FLT）的5'-O-酯前药：合成与抗HIV活性

5'-O-ester prodrugs of potent and selective anti-HIV agent--2',3'-dideoxy-3'-fluoro-2-thiothymidine (S2FLT): synthesis and anti-HIV activity.

作者信息

Miazga A, Poopeiko N E, Piasek A, Siweckar M A, Kulikowski T

机构信息

Institute of Biochemistry and Biophysics, Polish Academy of Sciences, Warszawa, Poland.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):805-7. doi: 10.1081/NCN-120022639.

DOI:10.1081/NCN-120022639
PMID:14565283
Abstract

Novel synthesis of 2',3'-dideoxy-3'-fluoro-2-thiothymidine (SFLT) based on transformation of appropriately protected 1-beta-D-threo-ribofuranosylthymine is presented. The synthesis and evaluation of SFLT 5'-O-ester prodrugs enzymatic hydrolysis, as well as their anti-HIV activity, is also described.

摘要

介绍了基于适当保护的1-β-D-苏型呋喃核糖基胸腺嘧啶转化的新型2',3'-二脱氧-3'-氟-2-硫代胸腺嘧啶（SFLT）合成方法。还描述了SFLT 5'-O-酯前药的合成、酶促水解评估及其抗HIV活性。

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