Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs

被引：8

作者：

Asai, A

Nagamura, S

Kobayashi, E

Gomi, K

Saito, H

机构：

[1] Kyowa Hakko Kogyo Co Ltd, Tokyo Res Labs, Tokyo 1948533, Japan

[2] Kyowa Hakko Kogyo Co Ltd, Pharmaceut Res Labs, Shizuoka 4118731, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(99)00518-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The water-soluble duocarmycin B1 prodrugs such as glycoside 3, phosphate 4 and carbamate 5 were synthesized for improving biological and pharmaceutical profiles of duocarmycin. Among these prodrugs, N-methylpiperazinylcarbamoyl derivative 5 exhibited potent antitumor activity against several human tumors in vivo. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：2995 / 2998

页数：4

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