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Anti-human immunodeficiency virus type 1 activities of dideoxynucleoside phosphotriester derivatives in primary
C Thumann-Schweitzer1, G Gosselin, C Périgaud
1Institut de Virologie de la Faculté de Médecine de Strasbourg, Unité INSERM 74, France.
Abstract:
Mononucleoside phosphotriester derivatives of dideoxynucleosides, following intracellular enzymatic activation, are likely to liberate their parent 5'-nucleoside monophosphate. Prodrugs of 3'-azido-2',3'-dideoxythymidine (AZT), 2',3'-didehydro-2',3'- dideoxythymidine (d4T), 2',3'-dideoxyinosine (ddl) and 2',3'-dideoxyadenosine (ddA) were evaluated for their anti-HIV1 activities in monocyte-derived macrophages, cells which are known to have low levels of nucleoside kinases. Prodrugs were found to be much more active, or just as active, as the corresponding dideoxynucleoside. Furthermore, their selectivity index was enhanced by a factor of 2 to 200.