Literature DB >> 1710021

[Suppression of the human immunodeficiency virus in cultured cells by 5'-phosphites of 3'-azido-2',3'-dideoxynucleosides].

E V Karamov, V V Lukashov, N B Tarusova, G V Kornilaeva, M A Rodova, M K Kukhanova, A A Kraevskiĭ.   

Abstract

5'-Phosphites (5'-hydrogenphosphonates) of 3'-azido-2'-, 3'-dideoxynucleosides are shown to be effective inhibitors of the human immunodeficiency virus (HIV-1) in MT4 cell culture. 5'-Phosphite of 3'-azido-2', 3'-dideoxythymidine was the most active among these compounds and even a little more active as compared to the well-known anti-AIDS drug 3'-azido-2',3'-dideoxythymidine; at the same time 5'-phosphites of 3'-azido-2',3' -dideoxynucleosides with adenine, guanine and cytosine bases were more active than the corresponding nucleosides. The toxicity of all four phosphites was comparatively low and the equimolar mixture of all four phosphites was 2-3 fold less toxic than each of them separately. Data on the decreased toxicity of the phosphite mixture are explained from the viewpoint of a decreased pool disbalance of natural 2'-deoxynucleoside 5'-triphosphates in cells; a significant pool disbalance is developed in the case of 3'-azido-2',3'-dideoxythymidine action.

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Year:  1990        PMID: 1710021

Source DB:  PubMed          Journal:  Mol Biol (Mosk)        ISSN: 0026-8984


  1 in total

1.  Formation of phosphonester bonds catalyzed by DNA polymerase.

Authors:  L S Victorova; N B Dyatkina; A M Atrazhev; A A Krayevsky; M K Kukhanova
Journal:  Nucleic Acids Res       Date:  1992-02-25       Impact factor: 16.971

  1 in total

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