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

Authors
Egron, D Arzumanov, AA Dyatkina, NB Krayevsky, A Imbach, JL Aubertin, AM Gosselin, G Perigaud, C
Citation
D. Egron et al., Synthesis, anti-HIV activity and stability studies of 3 '-azido-2 ',3 '-dideoxythymidine 5 '-fluorophosphate, NUCLEOS NUC, 18(4-5), 1999, pp. 983-984
Citations number
3
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES & NUCLEOTIDES
ISSN journal
07328311 → ACNP
Volume
18
Issue
4-5
Year of publication
1999
Pages
983 - 984
Database
ISI
SICI code
0732-8311(1999)18:4-5<983:SAAASS>2.0.ZU;2-A
Abstract
The synthesis, in vitro anti-HIV activity, and stability studies of AZT 5'- fluorophosphate (F-AZTMP) are reported. The present results demonstrate tha t such compound is a bioprecursor of its parent 5'-mononucleotide (AZTMP) b ut its biotransformation does not allow its selective intracellular deliver y. Moreover, several attempts were carried out in order to improve the biol ogical activity of this compound by the use of a SATE prodrug strategy.