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

来源：

ANTIVIRAL RESEARCH | 2006年 / 71卷 / 2-3期

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

页码：282 / 292

页数：11

共 38 条

[1] Intracellular metabolism of CycloSaligenyl 3′-azido-2′,3′-dideoxythymidine monophosphate, a prodrug of 3′-azido-2′,3′-dideoxythymidine (zidovudine) [J].