title: Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture.
abstract: Simple mono-derivatisation of the aryl moiety of some phosphoramidate pronucleotide 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.
authors.affiliation: Welsh School of Pharmacy, Cardiff University, UK.
authors.forename: A Q
authors.initials: AQ
authors.lastname: Siddiqui
authors.forename: C
authors.initials: C
authors.lastname: McGuigan
authors.forename: C
authors.initials: C
authors.lastname: Ballatore
authors.forename: O
authors.initials: O
authors.lastname: Wedgwood
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
authors.forename: J
authors.initials: J
authors.lastname: Balzarini
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D002478:Cells, Cultured; D016048:Dideoxyadenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D015498:HIV-2 / Q000187:drug effects; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D016048:Dideoxyadenosine; C075923:2'3'-didehydro-2'3'-dideoxyadenosine