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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:
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.
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页码:1219 / 1228
页数:10
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