Bioorganic & medicinal chemistry

Discovery of novel 4-anilinoquinazoline derivatives as potent inhibitors of epidermal growth factor receptor with antitumor activity

YY Xu, SN Li, GJ Yu, QH Hu, HQ Li

Index: Xu, Yun-Yun; Li, Si-Ning; Yu, Gao-Jian; Hu, Qing-Hua; Li, Huan-Qiu Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 19 p. 6084 - 6091

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Citation Number: 15

Abstract

Abstract Two new series of new compounds containing a 6-amino-substituted group or 6- acrylamide-substituted group linked to a 4-anilinoquinazoline nucleus have been discovered as potential EGFR inhibitors. These compounds proved efficient effects on antiproliferative activity and EGFR–TK inhibitory activity. Especially, N 6-((5-bromothiophen- 2-yl) methyl)-N 4-(3-chlorophenyl) quinazoline-4, 6-diamine (5e), showed the most potent ...