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New 5'-phosphonates, modified through the nucleoside sugar residue, as inhibitors of HIV replication

Kraevskiĭ, A.; Tarusova, N.; Zhu, K.I.; Vidal, P.; Chu, T.C.; Pol'ski, B.; Iang, K.I.; Matulich-Adamich, I.; Rozenberg, I.; Vatanabe, K.A.

Molekuliarnaia Biologiia 26(3): 624-634

1992

ISSN/ISBN: 0026-8984
PMID: 1406617
Document Number: 397845
A number of nucleoside 5'-phosphonates and nucleoside 5'-methylphosphonates were synthesised, to study their ability to inhibit reproduction of HIV-1. Three compounds, 5'-hydrogen phosphonates of 3'-azido-2',3'-dideoxythymidine (AZT-HP, IVc), 3'-fluoro-2',3'-dideoxythymidine (FLT-HP, IVa) and 2',3'-dideoxyadenosine (ddA-HP, I), exhibit potent anti-HIV-1 activity with selectivity indices similar to or better of those of their parent nucleosides.

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