Synthesis and biological evaluation of N-(7-indolyl)-3-pyridinesulfonamide derivatives as potent antitumor agents

被引：19

作者：

Owa, T ^{[1
]}

Yoshino, H ^{[1
]}

Okauchi, T ^{[1
]}

Okabe, T ^{[1
]}

Ozawa, Y ^{[1
]}

Sugi, NH ^{[1
]}

Yoshimatsu, K ^{[1
]}

Nagasu, T ^{[1
]}

Koyanagi, N ^{[1
]}

Kitoh, K ^{[1
]}

机构：

[1] Eisai & Co Ltd, Tsukuba Res Labs, Tsukuba, Ibaraki 3002635, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(02)00376-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We herein report the synthesis and antitumor activity of E7070 analogues containing a 3-pyridinesulfonamide moiety. E7070 was selected from our sulfonamide-based compound collections, currently undergoing Phase 11 clinical trials because of its tolerable toxicity profile and some antitumor responses in the Phase I setting. Of the analogues examined, ER-35745, a 6-amino-3-pyridinesulfonamide derivative, demonstrated significant oral efficacy against the HCT116 human colon carcinoma xenograft in nude mice. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2097 / 2100

页数：4

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