氟化无环核苷及其磷酰胺的合成及抗病毒评价

Nucleosides, Nucleotides and Nucleic Acids Pub Date : 2017-01-02 DOI:10.1080/15257770.2016.1218023

S. Mahmoud, Hao Li, Tamara R. Mcbrayer, L. Bassit, S. Hammad, S. Coats, F. Amblard, R. Schinazi

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引用次数: 1

摘要

摘要以市售的2,2,3,3-四氟-1,4-丁二醇和2,2,3,3,4,4-六氟-1,5-戊二醇为原料，经4 ~ 6步合成了一系列新的四氟和六氟无环核苷及其磷酰胺。评估了它们阻断HIV、HCV、HSV-1和HBV复制的能力，以及它们对HepG2、人淋巴细胞、CEM和Vero细胞的细胞毒性。

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Synthesis and antiviral evaluation of fluorinated acyclo-nucleosides and their phosphoramidates

ABSTRACT A novel series of tetrafluoro and hexafluoro acyclic nucleosides and their phosphoramidates were successfully prepared from commercially available 2,2,3,3-tetrafluoro-1,4-butanediol and 2,2,3,3,4,4-hexafluoro-1,5-pentanediol in four to six steps. Their ability to block HIV, HCV, HSV-1, and HBV replication along with their cytotoxicity toward HepG2, human lymphocyte, CEM, and Vero cells was assessed.

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Nucleosides, Nucleotides and Nucleic Acids

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