Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-L-glutamic acid diethyl ester:: Evaluation of in vitro anti-cancer and anti-folate activities

被引：11

作者：

Corona, Paola ^{[1
]}

Loriga, Mario ^{[1
]}

Costi, M. Paola ^{[2
]}

Ferrari, Stefania ^{[2
]}

Paglietti, Giuseppe ^{[1
]}

机构：

[1] Univ Sassari, Dipartimento Farmaco Chim Tossicol, I-07100 Sassari, Italy

[2] Univ Modena, Dipartimento Sci Farmaceut, I-41100 Modena, Italy

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 01期

关键词：

5,7-diaminoquinoxaline; ovarian carcinoma; leukemia; anti-folate;

D O I：

10.1016/j.ejmech.2007.03.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several diamino quinoxalines were designed, synthesized and evaluated as anti-tumor agents. Two compounds showed the most potent cytotoxic activities against the leukemia CCRF-CEM cell line (GI(50) < 0-01 mu M) and the ovarian cancer cell line OVCAR-4 (GI(50) = 0.03 mu M), respectively, with comparable/better activities than Methotrexate (MTX). Docking calculations of the complexes of hDHFR with the most active compounds identified the binding mode of the described molecules with respect to MTX. (C) 2007 Elsevier Masson SAS. All rights reserved.

引用

页码：189 / 203

页数：15

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