Synthesis and antitumor activity of duocarmycin derivatives:: A-ring pyrrole compounds bearing (β-(5′,6′,7′-trimethoxy-2′-indolyl)acryloyl group

被引：24

作者：

Amishiro, N ^{[1
]}

Nagamura, S ^{[1
]}

Kobayashi, E ^{[1
]}

Okamoto, A ^{[1
]}

Gomi, K ^{[1
]}

Okabe, M ^{[1
]}

Saito, H ^{[1
]}

机构：

[1] Kyowa Hakko Kogyo Co Ltd, Pharmaceut Res Inst, Nagaizumi, Shizuoka 4118731, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2000年 / 8卷 / 07期

关键词：

D O I：

10.1016/S0968-0896(00)00086-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of A-ring pyrrole derivatives of duocarmycin bearing beta-(5',6',7'-trimethoxy-2'-indolyl)acryloyl group were synthesized, and evaluated for in vitro anticellular activity against HeLa Sg cells and in vivo antitumor activity against murine sarcoma 180 in mice. New Seg-B analogues bearing beta-(5',6',7'-trimethoxy-2'-indolyl)acryloyl group containing double bond as spacer had lower peripheral blood toxicity than the derivatives bearing S',6',7'-trimethoxyindole-2'-carboxyl group in Seg-B of the natural type. Moreover, most of them exhibited potent antitumor activity against in vivo murine tumor models. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1637 / 1643

页数：7

共 42 条

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