SYNTHESIS OF THE PHOSPHODIESTER OF 3-BETA(7-BETA-HYDROXYCHOLESTEROL) AND OF 5'(3'DEOXY, 3'AZIDO-THYMIDINE)

Authors
PANNECOUCKE X PARMENTIER G SCHMITT G DOLLE F LUU B
Citation
X. Pannecoucke et al., SYNTHESIS OF THE PHOSPHODIESTER OF 3-BETA(7-BETA-HYDROXYCHOLESTEROL) AND OF 5'(3'DEOXY, 3'AZIDO-THYMIDINE), Tetrahedron, 50(4), 1994, pp. 1173-1178
Citations number
25
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron → ACNP
ISSN journal
00404020
Volume
50
Issue
4
Year of publication
1994
Pages
1173 - 1178
Database
ISI
SICI code
0040-4020(1994)50:4<1173:SOTPO3>2.0.ZU;2-G
Abstract
In order to enhance the therapeutic efficacy of azido-thymidine (AZT) by improving its pharmacokinetic properties and to try to target its a ction to the lymphocytes, the phosphodiester of 3 beta(7 beta-hydroxyc holesterol) and of 5'(3'deoxy, 3'azido-thymidine) 1 was synthesized us ing two different techniques of phosphorylation : the phosphoramidite and the hydrogen phosphonate methodologies. Preliminary results show a n in vitro anti-HIV activity.