Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines
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- 作者：Haiqing Yua ; 1 ; Yanxia Lib ; 1 ; Yang Gea ; Zhendong Songa ; Changyuan Wanga ; Shanshan Huanga ; Yue Jina ; Xu Hana ; Yuhong Zhena ; Kexin Liua ; kexinliu@dlmedu.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Youwen Zhouc ; youwen.zhou@ubc.ca" class="auth_mail" title="E-mail the corresponding author ; Xiaodong Maa ; xiaodong.ma@139.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：NSCLC ; EGFR ; T790M ; Quinazoline ; Adamantyl
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：3 March 2016
- 年：2016
- 卷：110
- 期：Complete
- 页码：195-203
- 全文大小：1449 K
文摘
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Quinazoline derivatives bearing an adamantyl group at the aniline ring were identified as potential EGFR inhibitors.
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Several analogues exhibited higher anti-tumor potency than gefitinib.
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Compound 3d displayed moderate activity against H1975 cells harboring the EGFRT790M mutation.