Novel antitumor 2-cyanoaziridine-1-carboxamides

被引：21

作者：

Iyengar, BS

Dorr, RT

Alberts, DS

Hersh, EM

Salmon, SE

Remers, WA ^{[1
]}

机构：

[1] Univ Arizona, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA

[2] Univ Arizona, Arizona Canc Ctr, Tucson, AZ 85721 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1999年 / 42卷 / 03期

关键词：

D O I：

10.1021/jm980600x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A set of 20 2-cyanoaziridine-1-carboxamides was synthesized from 2-cyanoaziridine and appropriate isocyanates. These compounds were active against a variety of solid and hematological tumor cells in culture, including strains resistant to doxorubicin and mitoxantrone. Their potencies in these assays correlated with the lipophilicity of substituents. The N-phenyl derivative was more potent and equally effective to imexon, a cyclized 2-cyanoaziridine-1-carboxamide of clinical interest, against cloned fresh human tumors.

引用

页码：510 / 514

页数：5

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