ADA-bypass by lipophilic cycloSal-ddAMP pro-nucleotides a second example of the efficiency of the cycloSal-concept

被引:34
作者
Meier, C [1 ]
Knispel, T [1 ]
DeClercq, E [1 ]
Balzarini, J [1 ]
机构
[1] CATHOLIC UNIV LEUVEN,REGA INST MED RES,B-3000 LOUVAIN,BELGIUM
关键词
D O I
10.1016/S0960-894X(97)00265-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of lipophilic pro-nucleotides of ddAMP 2 based on cycloSal-ddAMP 3a-c is described. Phosphotriesters 3 released ddAMP 2 selectively by a controlled, chemically induced tandem reaction. CycloSal-phosphotriesters 3 exhibited antiviral activity against HIV-1/HIV-2 in CEM cells that where by a factor up to hundred higher as compared to ddA 1. (C) 1997 Elsevier Science Ltd.
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页码:1577 / 1582
页数:6
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