[Study of anti-HIV activity of azidothymidine and fluorothymidine 5'-phosphonates].

It was established that 5'-phosphonates of 3'-azido-2',3'-dideoxythymidine (AZT) inhibit HIV reproduction in the MT-4 cell line as well as AZT. However, the viability of HIV-infected MT-4 cells after treatment with phosphonates was considerable higher that after AZT treatment. Inhibitory activities of 5'-phosphonates of 3'-fluoro-2',3'-dideoxythymidine (FLT) on HIV-infected MT-4 cells were rather low.

[4'-Branched nucleosides. I. Synthesis of 3'-deoxy-3'-amino-4'-hydroxymethylnucleosides].

The condensation of 1, 2-di-O-acetyl-3-azido-3-deoxy-4-benzoyloxymethyl-1-5-O-benzoyl-bet a-D-ribofuranose with trimethylsilyl derivatives of N6-benzoyladenine, N4-acetylcytosine and uracil in the presence of stannic chloride led to the corresponding nucleosides. After deprotection with methanolic ammonia the azidonucleosides were reduced with PPh3 into 3'-amino-3'-deoxy-4'-hydroxymethynucleosides.

[Synthesis of nucleoside analogs containing a cis-2-pentene fragment and their triphosphates].

Acyclic analogs of thymidine, adenine, and cytosine where the ribose moiety is replaced with cis-5-hydroxypenthene, were obtained via condensation of cis-5-acetoxy-1-bromo-2-pentene with nucleic acid bases. Triphosphate derivatives of the new nucleosides were also synthesized to evaluate their action as terminators of DNA synthesis catalyzed by DNA polymerases.