Synthesis and biological activity of 5-substituted anti-constrained acyclic analogs of cytidine and uridine

被引：7
|
作者：
Hsu, LY [1 ]
Chang, YM [1 ]
Lin, CH [1 ]
Drach, JC [1 ]
机构：
[1] UNIV MICHIGAN,SCH DENT,DEPT BIOL & MAT SCI,ANN ARBOR,MI 48109
来源：
NUCLEOSIDES & NUCLEOTIDES | 1996年 / 15卷 / 11-12期
关键词：
D O I：
10.1080/07328319608002736
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 number of 5-substituted constrained acyclic analogs of cytidine and uridine have been prepared in which the glycosyl torsion angle is constrained in the anti conformation. Compounds 2a-c, 3a-c, 4, 5 and 6 were tested for activity against HCMV and HSV-1. Compounds 2a and 2b showed moderate activity against HCMV. Compound 2c exhibited a weak inhibitory activity against HSV-1. Compounds 2a, 3a,4, 5, 6, 8, and 9 were screened for their anti-HIV or antitumor activity. None of them were active against HIV. However, compound 9 showed a 50% inhibition on MDA-MB-231/ATTC breast cancer cell growth at a concentration of 0.15 mu M.
引用
收藏
页码：1835 / 1847
页数：13
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