2008

Anticarcinogenic activityX 0070 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 Anticancer and Antifolate Activities. — Several diamino quinoxalines (I) are designed, synthesized, and evaluated as anti-tu-mor agents. Two compounds (Ia) and (Ib) show the most potent cytotoxic activities against the leukemia CCRF-CEM cell line and the ovarian cancer cell line OVCAR-4, respectively, with comparable/better activities than Methotrexate (MTX). Docking cal-culations of the complexes of hDHFR with the most active compounds identify the binding mode with respect to MTX. — (CORONA*, P.; LORIGA, M.; COSTI, M. P.; FERRARI, S.; PAGLIETTI, G.; Eur. J. Med. Chem. 43 (2008) 1, 189-203; Dip. Farm. Chim. Tossicol., Univ. Sassari, I-07100 Sassari, Italy; Eng.) — H. Haber

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