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异头糖硼酸类似物作为硼中子俘获治疗的潜在药物。

Anomeric sugar boronic acid analogues as potential agents for boron neutron capture therapy.

作者信息

Imperio Daniela, Del Grosso Erika, Fallarini Silvia, Lombardi Grazia, Panza Luigi

机构信息

Department of Pharmaceutical Sciences, Università del Piemonte Orientale, Largo Donegani 2, 28100 Novara, Italy.

出版信息

Beilstein J Org Chem. 2019 Jun 19;15:1355-1359. doi: 10.3762/bjoc.15.135. eCollection 2019.

Abstract

After the development of accelerators as neutron source, the access to new suitable agents for boron neutron capture therapy (BNCT) became a major need. Among many others, sugar boronic acids have recently attracted attention as boron carriers. Herein we report the synthesis and preliminary biological studies of two new sugar analogues containing a boronic acid at the anomeric position. The analogues were obtained by hydroboration of proper open-chain terminal alkenes that, after quenching with water, spontaneously afforded cyclic boronic acids with hemiacetal-like structures.

摘要

在加速器作为中子源得到发展之后,寻找用于硼中子俘获疗法(BNCT)的新型合适药物成为了一项主要需求。在众多物质中,糖硼酸最近作为硼载体引起了关注。在此,我们报告了两种在异头位置含有硼酸的新型糖类似物的合成及初步生物学研究。这些类似物是通过对适当的开链末端烯烃进行硼氢化反应得到的,烯烃经水淬灭后,自发形成具有半缩醛样结构的环状硼酸。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4dbb/6604725/e9fb0a6aa021/Beilstein_J_Org_Chem-15-1355-g002.jpg

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