Simple mono-derivatisation of the aryl moiety of d4A and ddA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture.

Authors
Siddiqui, AQ McGuigan, C Ballatore, C Wedgwood, O De Clercq, E Balzarini, J
Citation
Aq. Siddiqui et al., Simple mono-derivatisation of the aryl moiety of d4A and ddA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture., BIOORG MED, 9(17), 1999, pp. 2555-2560
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
17
Year of publication
1999
Pages
2555 - 2560
Database
ISI
SICI code
0960-894X(19990906)9:17<2555:SMOTAM>2.0.ZU;2-C
Abstract
Simple mono-derivatisation of the aryl moiety of some phosphoramidate pronu cleotide derivatives of d4A and ddA served to increase the lipophilicity of these membrane-soluble prodrugs. A concomitant and significant enhancement of potency against HIV-1 and HIV-2 in vitro was observed for the ddA- and d4A-based prodrugs compared to the original underivatised prodrugs. (C) 199 9 Elsevier Science Ltd. All rights reserved.