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Synthesis and biological evaluation of polyaminated 2',3'-dideoxy-3'-thiacytidine prodrugs
M Camplo1, N Mourier, J C Chermann
1Laboratoire de Chimie Biomoléculaire, INSERM U 322, Université de la Méditerrannée, Faculté des Sciences de Luminy, Marseille, France.
Nucleosides & Nucleotides
|August 5, 1999
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.