Application of the cycloSal-prodrug approach for improving the biological potential of phosphorylated biomolecules

被引:58
作者
Meier, C.
Balzarini, J.
机构
[1] Univ Hamburg, Inst Organ Chem, D-20146 Hamburg, Germany
[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
关键词
nucleoside analogs; antiviral agent; cycloSal-pronucleotides; carbohydrate drugs;
D O I
10.1016/j.antiviral.2006.04.011
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Pronucleotides represent a promising tool to improve the biological activity of nucleoside analogs in antiviral and cancer chemotherapy. The cycloSal-approach is one of several conceptually different pronucleotide systems. This approach can be applied to various nucleoside analogs. A salicyl alcohol as a cyclic bifunctional masking unit is used, and shown to afford a chemically driven release of the particular nucleotide from the lipophilic phosphate triester precursor molecule. A conceptual extension of the cycloSal-approach results in the design of "lock-in"-cycloSal-derivatives. The cycloSal-approach is not restricted to the delivery of bioactive nucleotides but also useful for the intracellular delivery of hexose-1-phosphates. (c) 2006 Elsevier B.V. All rights reserved.
引用
收藏
页码:282 / 292
页数:11
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