Novel cyclopropapyrroloindole derivative (AT-3510) bearing methoxycarbonyl and trifluoromethyl groups

被引：37

作者：

Fukuda, Y

Furuta, H

Kusama, Y

Ebisu, H

Oomori, Y

Terashima, S ^{[1
]}

机构：

[1] Kyorin Pharmaceut Co Ltd, Cent Res Labs, Nogi, Tochigi 3290114, Japan

[2] Sagami Chem Res Ctr, Kanagawa 2290012, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1999年 / 42卷 / 08期

关键词：

D O I：

10.1021/jm980668c

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The seco-Cl 3-methoxycarbonyl-2-trifluoromethylcyclopropapyrroloindole (MCTFCPI) derivatives dl- and/or (S)-10 carrying various acyl moieties at the NG-position were synthesized along with their prodrugs (S)-12, and their antitumor activity was evaluated. Among these derivatives, AT-3510 [(S)-12m], the novel prodrug MCTFCPI derivative carrying a 5-(7-methoxybenzofuran-2-ylcarbonyl)aminoindole-2-carbonyl group at the NG-position, was found to exhibit more excellent antitumor activity against human tumor xenografts than the clinical trial candidates carzelesin (6) and KW-2189 (7) and cisplatin.

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页码：1448 / 1458

页数：11

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