Synthesis of phosphorothioate analogues of oligodeoxyribonucleotides and their antiviral activity against human immunodeficiency virus (HIV). NLM AIDSLINE Important note: Information in this article was accurate in 1989. The state of the art may have changed since the publication date.

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Synthesis of phosphorothioate analogues of oligodeoxyribonucleotides and their antiviral activity against human immunodeficiency virus (HIV).

Gene. 1988 Dec 10;72(1-2):343-7. Unique Identifier : AIDSLINE MED/89211930
Matsukura M; Zon G; Shinozuka K; Stein CA; Mitsuya H; Cohen JS; Broder S; Clinical Oncology Program, National Cancer Institute, Bethesda,; MD 20892.

Abstract: Nuclease-resistant phosphorothioate analogues of oligodeoxynucleotides (oligos) were synthesized by sulfurization of either internucleoside phosphite linkages, in a repetitive manner during chain extension, or internucleoside hydrogen phosphonate linkages, in a single step following chain assembly. These analogues were tested as antiviral agents against human immunodeficiency virus (HIV). In a cytopathic effect inhibition assay using HIV-uninfected susceptible T cells (tetanus toxoid-specific normal T cells) co-cultured with irradiated chronically HIV-infected cells, phosphorothioate oligomers inhibited the cytopathic effect and replication of several isolates of HIV-1 and HIV-2. Thus phosphorothioate analogues of oligos could inhibit cell-to-cell transmission of the virus as well as the infection by cell-free virus particles and also could inhibit a variety of isolates of human retroviruses.
Keywords: Antiviral Agents/*CHEMICAL SYNTHESIS Cell Line HIV/*DRUG EFFECTS/PHYSIOLOGY Indicators and Reagents Oligodeoxyribonucleotides/*CHEMICAL SYNTHESIS/PHARMACOLOGY Structure-Activity Relationship Thionucleotides/*CHEMICAL SYNTHESIS/PHARMACOLOGY Virus Replication/DRUG EFFECTS JOURNAL ARTICLE

KWDantiviralagents/KWDchemicalsynthesiscelllinehiv/KWDdrugeffects/physiologyindicatorsandreagentsoligodeoxyribonucleotides/KWDchemicalsynthesis/pharmacologystructure-activityrelationshipthionucleotides/KWDchemicalsynthesis/pharmacologyvirusreplication/drugeffectsjournalarticle
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M8980794

Copyright © 1989 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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