SYNTHESIS AND ANTI-HIV ACTIVITY OF 3'-O-FORMYL DERIVATIVES OF THYMIDINE AND 2'-DEOXYURIDINE

被引:3
|
作者
KUMAR, R [1 ]
KNAUS, EE [1 ]
WIEBE, LI [1 ]
机构
[1] UNIV ALBERTA,FAC PHARM & PHARMACEUT SCI,EDMONTON T6G 2N8,ALBERTA,CANADA
来源
NUCLEOSIDES & NUCLEOTIDES | 1992年 / 11卷 / 06期
基金
英国医学研究理事会;
关键词
D O I
10.1080/07328319208018337
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
Reaction of the 5'-O-t-butyldimethylsilyl derivatives of thymidine and 2'-deoxyuridine with the Vilsmeier reagent (POCl3/DMF), and removal of the t-butyldimethylsilyl protecting group, afforded 3'-O-formylthymidine (5) and 3'-O-formyl-2'-deoxyuridine (6), respectively. In vitro evaluation, determined as the ability of the test compound to inhibit HIV induced cytopathogenicity in CEM cells, indicated that 5 was moderately active, whereas 6 was inactive.
引用
收藏
页码:1219 / 1228
页数:10
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