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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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.
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