Takahashi T, Tanaka H, Matsuda A, Doi T, Yamada H
Department of Chemical Engineering, Tokyo Institute of Technology, Japan.
Bioorg Med Chem Lett. 1998 Dec 1;8(23):3299-302. doi: 10.1016/s0960-894x(98)00605-2.
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.
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。