Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents

QZ Zheng, F Zhang, K Cheng, Y Yang, Y Chen…

Index: Zheng, Qing-Zhong; Zhang, Fei; Cheng, Kui; Yang, Ying; Chen, Yu; Qian, Yong; Zhang, Hong-Juan; Li, Huan-Qiu; Zhou, Chang-Fang; An, Shu-Qing; Jiao, Qing-Cai; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 2 p. 880 - 886

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Citation Number: 18

Abstract

A series of amide-coupled benzoic nitrogen mustard derivatives as potential EGFR and HER- 2 kinase inhibitors were synthesized and reported for the first time. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Of all the studied compounds, compounds 5b and 5t exhibited the most potent inhibitory activity, which was comparable to the positive control erlotinib. Docking simulation was performed to position compounds 5b and 5t into ...