Potent inhibition of hepatitis B virus production in vitro by modified pyrimidine nucleosides. NLM AIDSLINE Important note: Information in this article was accurate in 1991. The state of the art may have changed since the publication date.

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Potent inhibition of hepatitis B virus production in vitro by modified pyrimidine nucleosides.

Antimicrob Agents Chemother. 1990 Oct;34(10):1986-90. Unique Identifier : AIDSLINE MED/91151061
Matthes E; Langen P; von Janta-Lipinski M; Will H; Schroder HC; Merz H; Weiler BE; Muller WE; Zentralinstitut fur Molekularbiologie, Akademie der; Wissenschaften der Deutschen Demokratischen Republik,; Berlin-Buch, German Democratic Republic.

Abstract: 2',3'-Dideoxy-3'-fluorothymidine (FddThd), 2',3'-didehydro-2',3'- dideoxythymidine (ddeThd), and 3'-fluoro-5-methyl-deoxycytidine (FddMeCyt) are, in their triphosphate forms, selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase. We report that 0.3 microM FddThd, FddMeCyt, or ddeThd as well as 3'-chloro-5-methyl-deoxycytidine (ClddMeCyt) or 3'-amino-5-methyl-deoxycytidine (AddMeCyt) almost completely blocked production of hepatitis B virus (HBV) particles by HBV DNA-transfected cell line 2.2.15 in vitro. Only at an at least 10-fold-higher concentration was a cytotoxic effect observed. These results indicate that FddThd, FddMeCyt, ClddMeCyt, AddMeCyt, and ddeThd are potent anti-HBV agents in vitro.
Keywords: Antiviral Agents/*PHARMACOLOGY Cell Division/DRUG EFFECTS Cell Line DNA Replication/DRUG EFFECTS DNA, Viral/*DRUG EFFECTS Hepatitis B Virus/*DRUG EFFECTS/PHYSIOLOGY Hybridization/DRUG EFFECTS Pyrimidine Nucleosides/*PHARMACOLOGY Support, Non-U.S. Gov't JOURNAL ARTICLEKWDantiviralagents/KWDpharmacologycelldivision/drugeffectscelllinednareplication/drugeffectsdna,viral/KWDdrugeffectshepatitisbvirus/KWDdrugeffects/physiologyhybridization/drugeffectspyrimidinenucleosides/KWDpharmacologysupport,non-uKWDsKWDgov'tjournalarticle
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M9160663

Copyright © 1991 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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