The synthesis and biological evaluation of sulfamoyl nucleosides related to carbovir and AZT

被引:5
作者
Vince, R
Pham, PT
机构
[1] Department of Medicinal Chemistry College of Pharmacy, S.E. University of Minnesota, Minneapolis, MN 55455-0343
来源
NUCLEOSIDES & NUCLEOTIDES | 1995年 / 14卷 / 9-10期
关键词
D O I
10.1080/15257779508010723
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
A series of 5'-(O) under bar-sulfamoylated carbocyclic 2',3'-dideoxy nucleosides was synthesized and evaluated for antitumor and anti-HIN activities. In this study, we have combined the phosphate mimicking features of the sulfamoyl group with our previously reported antiviral carbocyclic nucleoside, carbovir. In a related strategy, the sufamoyl moiety was used as a replacement for the alpha-phosphate of AZT-triphosphate in an analog designed to examine a membrane permeable HIV reverse transcriptase inhibitor. Some of the analogs exhibited significant in vitro anticancer activity.
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收藏
页码:2051 / 2060
页数:10
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