Synthesis of derivatives of NK109, 7-OH benzo[c]phenanthridine alkaloid, and evaluation of their cytotoxicities and reduction-resistant properties

被引：107

作者：

Nakanishi, T ^{[1
]}

Masuda, A ^{[1
]}

Suwa, M ^{[1
]}

Akiyama, Y ^{[1
]}

Hoshino-Abe, N ^{[1
]}

Suzuki, M ^{[1
]}

机构：

[1] Nippon Kayaku Co Ltd, Pharmaceut Grp, Kita Ku, Tokyo 1158588, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(00)00467-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The N-5-C-6 double bond of NK109 (an antitumor benzo[c]phenanthridine alkaloid) is easily reduced under biological environment. To suppress the inactivation caused by reduction, we synthesized 5-, 6-, and 8-substituted NK109. 5-Substituted derivatives (4a-c) were reduced more easily than NK109. 6-Substituted ones (10a-f) inhibited biological reduction, but showed weak cytotoxic activity. 8-O-Substituted ones (13a-h), especially 8-O-hydroxyethyl NK109 (13d), suppressed biological reduction and exhibited strong cytotoxic activity. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2321 / 2323

页数：3

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