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生物催化方法在核苷前药合成中的应用。

Biocatalytic approaches applied to the synthesis of nucleoside prodrugs.

机构信息

Laboratorio de Biocatálisis y Biotransformaciones, Departamento de Ciencia y Tecnología, Universidad Nacional de Quilmes, Roque Sáenz Peña 352, 1876 Bernal, Buenos Aires, Argentina.

Biocatalysis Group, Delft University of Technology, Julianalaan 67, 2628 BC Delft, The Netherlands.

出版信息

Biotechnol Adv. 2015 Sep-Oct;33(5):412-34. doi: 10.1016/j.biotechadv.2015.03.009. Epub 2015 Mar 18.

Abstract

Nucleosides are valuable bioactive molecules, which display antiviral and antitumour activities. Diverse types of prodrugs are designed to enhance their therapeutic efficacy, however this strategy faces the troublesome selectivity issues of nucleoside chemistry. In this context, the aim of this review is to give an overview of the opportunities provided by biocatalytic procedures in the preparation of nucleoside prodrugs. The potential of biocatalysis in this research area will be presented through examples covering the different types of nucleoside prodrugs: nucleoside analogues as prodrugs, nucleoside lipophilic prodrugs and nucleoside hydrophilic prodrugs.

摘要

核苷是具有生物活性的重要分子,具有抗病毒和抗肿瘤活性。设计了多种前药来提高它们的治疗效果,但这种策略面临核苷化学选择性的问题。在这种情况下,本综述的目的是概述生物催化方法在制备核苷前药方面提供的机会。通过涵盖不同类型核苷前药的例子,将展示生物催化在该研究领域的潜力:核苷类似物作为前药、核苷亲脂性前药和核苷亲水性前药。

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