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Synthesis, Anti-HIV Activity, and Stability Studies of 5′-Phosphorofluoridate Derivatives of AZT

✍ Scribed by D. Egron; A.A. Arzumanov; N.B. Dyatkina; A.-M. Aubertin; J.-L. Imbach; G. Gosselin; A. Krayevsky; C. Périgaud

Publisher
Elsevier Science
Year
2001
Tongue
English
Weight
134 KB
Volume
29
Category
Article
ISSN
0045-2068

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✦ Synopsis

The synthesis, in vitro anti-HIV activity and stability studies of the 5Ј-fluorophosphate derivative of 3Ј-azido-3Ј-deoxythymidine (AZT) are reported. The results support the hypothesis that this phosphorylated entity exerts its biological effect via the delivery of the corresponding 5Ј-mononucleotide through an enzymatic process. However, the antiviral evaluation in thymidine kinasedeficient CEM cells as well as the stability studies in culture medium and cell extract showed that this bioconversion is not specific to the intracellular medium. Attempts to improve the biological activity of mononucleoside 5Ј-fluorophosphates by the use of the S-pivaloyl-2-thioethyl (tBuSATE) group as biolabile phosphate protection are reported. ᭧ 2001 Elsevier Science (USA)

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