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具有DNA嵌入剂和糖部分的九元环掩蔽烯二炔类似物的合成。

Synthesis of 9-membered masked enediyne analogues possessing DNA intercalator and sugar moieties.

作者信息

Takahashi T, Tanaka H, Matsuda A, Doi T, Yamada H

机构信息

Department of Chemical Engineering, Tokyo Institute of Technology, Japan.

出版信息

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3299-302. doi: 10.1016/s0960-894x(98)00605-2.

Abstract

Syntheses of hybrid DNA cleaving molecules which have the 9-membered enediyne structure of kedarcidin with the DNA intercalator of NCS and/or the sugar moieties were accomplished. Introduction of the sugar moieties to the masked enediyne was achieved via S-alkylation of a bromoacetate derivative with a sugar-containing thiol without the need for protection of the sugar moiety.

摘要

成功合成了具有克氏菌素九元烯二炔结构并带有NCS的DNA嵌入剂和/或糖部分的杂合DNA切割分子。通过溴乙酸酯衍生物与含硫醇糖的S-烷基化反应,在无需保护糖部分的情况下,将糖部分引入到掩蔽的烯二炔中。

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