[Inhibition of HIV reproduction in cell culture by 5'-phosphonates of 3'-azido-2',3'-dideoxynucleosides].
The antiviral activity of 3'-azido-2',3'-dideoxynucleoside 5'-phosphate analogues: 5'-phosphonomethylene-3'-azido-2',3'-dideoxythymidine, 5'-methylphosphonate and 5'-phosphite of 3'-azido-2',3'-dideoxythymidine, 5'-phosphites of 3'-azido-2',3'-dideoxyadenosine and guanosine was investigated in HIV-infected cell cultures (human lymphoblastoid cells). The effectivity of inhibition of HIV-reproduction in cells by these substances was close or even higher than that for the corresponding 3'-azido-2',3'-dideoxynucleosides, whereas their toxicity was lower than that of nucleosides. These substances are supposed to be transported into the cells and to be transformed into the corresponding 5'-triphosphate analogues under the action of cell kinases. It is possible that such agents are terminator substrates of virus reverse transcriptases and thus inhibit the biosynthesis of DNA chains.
Tarusova
N B
NB
Khorlin
A A
AA
Kraevskiĭ
A A
AA
Korneeva
M N
MN
Nosik
D N
DN
Kruglov
I V
IV
Galegov
G A
GA
Bibilashvili
R Sh
RSh
D000998:Antiviral Agents / Q000138:chemical synthesis; D001386:Azides / Q000138:chemical synthesis / Q000494:pharmacology*; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002621:Chemistry; D016048:Dideoxyadenosine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D015224:Dideoxynucleosides / Q000138:chemical synthesis / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D063065:Organophosphonates / Q000138:chemical synthesis / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects*; D015215:Zidovudine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology
D000998:Antiviral Agents; D001386:Azides; D015224:Dideoxynucleosides; D063065:Organophosphonates; D015215:Zidovudine; D016048:Dideoxyadenosine; C051073:3'-azido-2',3'-dideoxyguanosine
Ingibirovanie reproduktsii virusa immunodefitsita cheloveka v kul'ture kletok 5'-fosfonatami 3'-azido-2',3'-dideoksinukleozidov.