Synthesis of novel quinoxaline derivatives and its cytotoxic activities

被引：58

作者：

Tanimori, Shinji ^{[1
]}

Nishimura, Takeshi ^{[1
]}

Kirihata, Mitsunori ^{[1
]}

机构：

[1] Osaka Prefecture Univ, Grad Sch Life & Environm Sci, Dept Biosci & Informat, Naka Ku, Osaka 5998531, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 15期

关键词：

Quinoxaline; Dihydroquinoxalin-2-one; Ullmann reaction; One-pot synthesis; Domino reaction; Cascade reaction; Cytotoxic activity; ANTAGONIST; RECEPTOR; AMINES;

D O I：

10.1016/j.bmcl.2009.06.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Substituted dihydroquinozalin-2-ones (1-16) have been synthesized easily by the use of copper-catalyzed coupling method. The reactions of 2-haloanilines with a variety of alpha-amino acids in the presence of copper (I) iodide gave corresponding 3-substituted dihydroquinozalin-2-ones in up to 86% yield. Some new quinoxalin-2-ones (2, 4, 5, 13 and 16) have moderate cytotoxic activity toward HeLaS3 cell lines at 4.9-18.1 mu M. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4119 / 4121

页数：3

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