Synthesis and antitumor activity of novel cyclopropapyrroloindole (CPI) derivatives bearing bis(methoxycarbonyl) groups

被引:9
作者
Fukuda, Y [1 ]
Oomori, Y [1 ]
Kusama, Y [1 ]
Terashima, S [1 ]
机构
[1] SAGAMI CHEM RES CTR, SAGAMIHARA, KANAGAWA 229, JAPAN
关键词
ANTI-TUMOR AGENT; DNA ALKYLATION; DUOCARMYCIN-A; STREPTOMYCES SP; CC-1065; ANALOGS; IDENTIFICATION; CYTOTOXICITY; ANTIBIOTICS; BINDING;
D O I
10.1016/S0960-894X(97)00099-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The title synthesis was achieved by employing oxidative cyclization of the enaminodiester prepared by Michael addition of the 5-aminoindoline with dimethyl acetylenedicarboxylate, as a key step. Some of these novel bis(methoxycarbonyl)cyclopropapyrroloindole (MC(2)CPI) derivatives 9c, d and their seco-chlorides 18c, d were found to exhibit prominent cytotoxicity and antitumor activity against P388 murine leukemia. (C) 1997 Elsevier Science Ltd.
引用
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页码:749 / 752
页数:4
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