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5'-(Z)-取代的4',5'-不饱和腺苷的立体定向合成及其对S-腺苷同型半胱氨酸水解酶抑制活性的评价。

Stereo-defined synthesis of 5'-(Z)-substituted 4',5'-unsaturated adenosines and evaluation of their inhibitory activity against S-adenosyl homocysteine hydrolase.

作者信息

Kumamoto Hiroki, Onuma Sayoko, Tanaka Hiromichi, Kitade Yukio

机构信息

School of Pharmaceutical Sciences, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan.

出版信息

Nucleic Acids Res Suppl. 2003(3):13-4. doi: 10.1093/nass/3.1.13.

DOI:10.1093/nass/3.1.13
PMID:14510356
Abstract

A new approach was developed for the synthesis of 5'-(Z)-substituted 4',5'-unsaturated adenosines, potential inhibitors against S-adenosyl-L-homocysteine hydrolase (SAHase). A highly stereoselective radical-mediated sulfur-extrusive stannylation was employed as a key step in the present approach. Inhibitory activity of the compounds against SAHase is also presented.

摘要

开发了一种合成5'-(Z)-取代的4',5'-不饱和腺苷的新方法,这些腺苷是针对S-腺苷-L-高半胱氨酸水解酶(SAHase)的潜在抑制剂。一种高度立体选择性的自由基介导的硫挤出锡化反应被用作本方法的关键步骤。还介绍了这些化合物对SAHase的抑制活性。

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