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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.
E V Karamov, and
V V Lukashov, and
N B Tarusova, and
G V Kornilaeva, and
M A Rodova, and
M K Kukhanova, and
A A Kraevskiĭ
May 1989,
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E V Karamov, and
V V Lukashov, and
N B Tarusova, and
G V Kornilaeva, and
M A Rodova, and
M K Kukhanova, and
A A Kraevskiĭ
January 2007,
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E V Karamov, and
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N B Tarusova, and
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A A Kraevskiĭ
January 1993,
Biochemical pharmacology,
E V Karamov, and
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N B Tarusova, and
G V Kornilaeva, and
M A Rodova, and
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January 1989,
Molekuliarnaia biologiia,
E V Karamov, and
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N B Tarusova, and
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September 1993,
Molecular pharmacology,
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A A Kraevskiĭ
June 1987,
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E V Karamov, and
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N B Tarusova, and
G V Kornilaeva, and
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A A Kraevskiĭ
October 1987,
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E V Karamov, and
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N B Tarusova, and
G V Kornilaeva, and
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M K Kukhanova, and
A A Kraevskiĭ
October 1988,
Molecular pharmacology,
E V Karamov, and
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M K Kukhanova, and
A A Kraevskiĭ
January 2006,
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