Synthesis and biological evaluation of polyaminated 2',3'-dideoxy-3'-thiacytidine prodrugs. |
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| Authors: | M Camplo N Mourier J C Chermann J L Kraus |
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| Affiliation: | Laboratoire de Chimie Biomoléculaire, INSERM U 322, Université de la Méditerrannée, Faculté des Sciences de Luminy, Marseille, France. |
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| Abstract: | The syntheses and biological evaluation of polyaminated 2',3'-dideoxy-3'-thiacytidine have been performed. A new lead was found to increase the in vitro antiviral potency (syncitia formation on MT-4 cell line) of two order magnitude greater than the parent nucleoside drug. Moreover, the in vitro activity on HIV macrophages was found to be more than 3 log greater than the activity of the parent drug 1. |
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