SYNTHESIS AND EVALUATION OF THE ANTITUMOR-ACTIVITY OF 4,5-DIAMINO-SUBSTITUTED 1,2-BENZOQUINONES

被引：22
|
作者：
HUANG, ZD [1 ]
CHEN, YN [1 ]
MENON, K [1 ]
TEICHER, BA [1 ]
机构：
[1] HARVARD UNIV,SCH MED,DANA FARBER CANC INST,44 BINNEY ST,BOSTON,MA 02115
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 13期
关键词：
D O I：
10.1021/jm00065a001
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 4,5-diamino-substituted-1,2-benzoquinones were prepared from catechol and the corresponding secondary amines in high yield in a single step using copper complex formation to stabilize the intermediate. The cytotoxicity of the products under various conditions was evaluated using the EMT-6 mammary carcinoma cell line, and antitumor activity was tested in the L1210 murine leukemia. The 4,5-diaziridinyl-1,2-benzoquinone was a more potent cytotoxic agent than diaziquone (AZQ) and was very effective against the L1210 leukemia. The azetidine, pyrrolidine, and diethylamine derivatives were not effective antitumor agents.
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收藏
页码：1797 / 1801
页数：5
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