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

被引:4
|
作者
Egron, D
Arzumanov, AA
Dyatkina, NB
Krayevsky, A
Imbach, JL
Aubertin, AM
Gosselin, G
Périgaud, C
机构
[1] Univ Montpellier 2, Lab Chim Biorgan, UMR CNRS USTL 5625, F-34095 Montpellier 5, France
[2] Russian Acad Sci, Engelhardt Inst Mol Biol, Moscow 117984, Russia
[3] Univ Strasbourg 1, Inst Virol, INSERM U74, F-67000 Strasbourg, France
来源
NUCLEOSIDES & NUCLEOTIDES | 1999年 / 18卷 / 4-5期
关键词
D O I
10.1080/15257779908041621
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:983 / 984
页数:2
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