Naphthazarin derivatives (II): Formation of glutathione conjugate, inhibition of DNA topoisomerase-I and cytotoxicity

被引：27

作者：

Song, GY ^{[1
]}

Zheng, XG ^{[1
]}

Kim, Y ^{[1
]}

You, YJ ^{[1
]}

Sok, DE ^{[1
]}

Ahn, BZ ^{[1
]}

机构：

[1] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(99)00397-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

6-(1-Hydroxyalkyl)-5,8-dimethoxy-1,4-naphthoquinones, expressing a higher reactivity in conjugation with glutathione, showed a greater potency in the inhibition of DNA topoisomerase-I and the cytotoxicity against L1210 cells than 2-(1-hydroxyalkyl)-DMNQ derivatives, implying the participation of electrophilic arylation in the bioactivities. In further study 6-(1-Hydroxyalkyl)-5,8-dimethoxy-1,4-naphthoquinones with an alkyl group of shorter chain length (C-2 similar to C-6) exerted a greater bioactivities than those with longer chain length(>C-6). (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2407 / 2412

页数：6

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