Bulletin of the Korean chemical society | |
Synthesis and Anti-HIV-1 Activity of Carbocyclic Versions of Stavudine Analogues Using a Ring-closing Metathesis | |
Joon Hee Hong1  Lian Jin Liu1  Ok Hyun Ko1  | |
关键词: Carbocyclic nucleoside; Antiviral agents; Ring-closing metathesis; Claisen rearrangement; | |
DOI : | |
学科分类:化学(综合) | |
来源: Korean Chemical Society | |
【 摘 要 】
An efficient synthetic route for carbocyclic versions of stavudine analogues and their evaluation on antiviral activity are described. The construction of an ethynylated quaternary carbon at the 4`-position of carbocyclic nucleosides was accomplished using Claisen rearrangement of 11 and ring-closing metathesis (RCM) of dienyne 14 as key transformations. An antiviral evaluation of the synthesized compounds, 20, 21, 22, and 25 against HIV-1, HSV-1, HSV-2, and HCMV showed that only the guanine analogue 25 is moderately active against HIV-1 in the MT-4 cell line (EC50 = 11.91 レmol).
【 授权许可】
Unknown
【 预 览 】
Files | Size | Format | View |
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RO201912010241141ZK.pdf | 234KB | download |