Synthesis of nucleotide analogues, EFdA, EdA and EdAP, and the effect of EdAP on hepatitis B virus replication

Autor: Kamata, Mai, Takeuchi, Toshifumi, Hayashi, Ei, Kazane Nishioka, Oshima, Mizuki, Iwamoto, Masashi, Nishiuchi, Kota, Kamo, Shogo, Shusuke Tomoshige, Watashi, Koichi, Kamisuki, Shinji, Ohrui, Hiroshi, Sugawara, Fumio, Kuramochi, Kouji
Rok vydání: 2019
DOI: 10.6084/m9.figshare.9944795.v1
Popis: 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.
Databáze: OpenAIRE