Synthesis of acylphosphates of purine ribonucleosides

被引:18
作者
Kreimeyer, A [1 ]
UghettoMonfrin, J [1 ]
Namane, A [1 ]
HuynhDinh, T [1 ]
机构
[1] INST PASTEUR,UNITE CHIM ORGAN,CNRS 487,F-75724 PARIS 15,FRANCE
关键词
D O I
10.1016/S0040-4039(96)02016-3
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Nucleotides do not penetrate cells at a sufficient rate to realize their therapeutic potential. To overcome this limitation we have envisaged acyl nucleodi(tri)phosphates (ND(T)Ps) as suitable membrane permeable prodrugs because a) preliminary experiences have shown that these compounds are preferably cleaved at their mixed carboxylic phosphoric bond to generate the corresponding carboxylic group (3) and nucleotides (2)(1), and b) the potential modification of the acyl group R allows to vary the lipophilicity of the acyl nucleotide derivative. Copyright (C) 1996 Published by Elsevier Science Ltd
引用
收藏
页码:8739 / 8742
页数:4
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