SYNTHESIS AND ANTI-HIV ACTIVITY OF 4′-MODIFIED CYCLOPENTENYL PYRIMIDINE C-NUCLEOSIDES

被引:5
|
作者
Liu, Lian Jin [1 ]
Hong, Joon Hee [1 ]
机构
[1] Chosun Univ, Coll Pharm, Project Team BK21, Kwangju 501759, South Korea
来源
关键词
Cyclopentenyl C-nucleoside; antiviral agents; S(N)2 alkylation; ANTIVIRAL ACTIVITY; ENANTIOSELECTIVE SYNTHESIS; CARBOCYCLIC ANALOGS; 9-DEAZAADENOSINE; ANTITUMOR; CYTIDINE;
D O I
10.1080/15257770902946058
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Novel syntheses of 4-modified cyclopentenyl pyrimidine C-nucleosides were performed via C-C bond formation using S(N)2 alkylation via the key intermediate mesylates 6 and 16, which were prepared,from acyclic ketone derivatives. When antiviral evaluation of synthesized, compound was performed against various viruses such as HIV-1, HSV-1 and HSV-2, isocytidine analogue 20 showed, moderate anti-HIV activity in CEM cell line (EC50 = 13.1 mu mol).
引用
收藏
页码:303 / 314
页数:12
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