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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

Corona, Paola and Loriga, Mario and Costi, M.Paola and Ferrari, Stefania and Paglietti, Giuseppe (2008) 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. European Journal of Medicinal Chemistry, Vol. 43 (1), p. 189-203. ISSN 0223-5234. Article.

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DOI: 10.1016/j.ejmech.2007.03.035

Abstract

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 (GI50 < 0.01 μM) and the ovarian cancer cell line OVCAR-4 (GI50 = 0.03 μM), 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.

Item Type:Article
ID Code:502
Status:Published
Refereed:Yes
Uncontrolled Keywords:5,7-Diaminoquinoxaline, ovarian carcinoma, leukemia, anti-folate
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Elsevier Masson
ISSN:0223-5234
Copyright Holders:© 2007 Elsevier Masson
Deposited On:18 Aug 2009 10:02

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