Synthesis and antitumor activity of duocarmycin derivatives: Modification at the C-7 position of segment-A of A-ring pyrrole compounds

被引：6

作者：

Amishiro, N ^{[1
]}

Okamoto, A ^{[1
]}

Okabe, M ^{[1
]}

Saito, H ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2000年 / 8卷 / 05期

关键词：

D O I：

10.1016/S0968-0896(00)00046-8

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 the C7-substituted A-ring pyrrole derivatives of duocarmycin were synthesized, and evaluated for in vitro anticellular activity against HeLa S-3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. All of the C7-substituted A-ring pyrrole compounds decreased potency in vitro and in vivo. However, some showed strong antitumor activity with T/C values less than 0.3. Among them, the 7-formyl compound 5d showed remarkable potent in vivo antitumor activity and low peripheral blood toxicity, which were equal to 2c. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1195 / 1201

页数：7

共 38 条

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