학술논문

Synthesis of nucleotide analogues, EFdA, EdA and EdAP, and the effect of EdAP on hepatitis B virus replication.
Document Type
Article
Source
Bioscience, Biotechnology & Biochemistry. Feb2020, Vol. 84 Issue 2, p217-227. 11p.
Subject
*HEPATITIS B virus
*NUCLEOTIDE synthesis
*VIRAL replication
*HIV
*REVERSE transcriptase
*INFLUENZA viruses
Language
ISSN
0916-8451
Abstract
4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) and 4′-ethynyl-2′-deoxyadenosine (EdA) are nucleoside analogues which inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. EdAP, a cyclosaligenyl (cycloSal) phosphate derivative of EdA, inhibits the replication of the influenza A virus. The common structural feature of these compounds is the ethynyl group at the 4′-position. In this study, these nucleoside analogues were prepared by a common synthetic strategy starting from the known 1,2-di-O-acetyl-D-ribofuranose. Biological evaluation of EdAP revealed that this compound reduced hepatitis B virus (HBV) replication dose-dependently without cytotoxicity against host cells tested in this study. Synthesis of nucleotide analogues, EFdA, EdA and EdAP, and the effect of EdAP on hepatitis B virus replication. [ABSTRACT FROM AUTHOR]