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Title: Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency
Authors: Cushman, M ×
Insaf, S
Paul, G
Ruell, J A
De Clercq, Erik
Schols, Dominique
Pannecouque, Christophe
Witvrouw, Myriam
Schaeffer, C A
Turpin, J A
Williamson, K
Rice, W G #
Issue Date: May-1999
Series Title: Journal of Medicinal Chemistry vol:42 issue:10 pages:1767-77
Abstract: The anti-HIV agent cosalane inhibits both the binding of gp120 to CD4 as well as an undefined postattachment event prior to reverse transcription. Several cosalane analogues having an extended polyanionic "pharmacophore" were designed based on a hypothetical model of the binding of cosalane to CD4. The analogues were synthesized, and a number of them displayed anti-HIV activity. One of the new analogues was found to possess enhanced potency as an anti-HIV agent relative to cosalane itself. Although the new analogues inhibited both HIV-1 and HIV-2, they were more potent as inhibitors of HIV-1 than HIV-2. Mechanism of action studies indicated that the most potent of the new analogues inhibited fusion of the viral envelope with the cell membrane at lower concentrations than it inhibited attachment, suggesting inhibition of fusion as the primary mechanism of action.
URI: 
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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