Design, Synthesis, and In vitro Antitumor Activity Evaluation of Novel 4??pyrrylamino Quinazoline Derivatives

X Wu, M Li, W Tang, Y Zheng, J Lian…

Index: Wu, Xiaoqing; Li, Mingdong; Tang, Wenhua; Zheng, Youguang; Lian, Jiqin; Xu, Liang; Ji, Min Chemical Biology and Drug Design, 2011 , vol. 78, # 6 p. 932 - 940

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Citation Number: 8

Abstract

Here, we describe the design and synthesis of two series of 4-pyrrylamino quinazolines as new analogs of the epidermal growth factor receptor inhibitor gefitinib. In vitro antitumor activity of these novel compounds against pancreatic (Miapaca2) and prostate (DU145) cancer cell lines was evaluated. Compared with the parental gefitinib, all 18 derivatives show a greatly increased cytotoxicity to cancer cells. In vitro kinase inhibitory activity on ...