Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold
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- 作者：Siyuan Yin ; Chunming Tang ; Bin Wang ; Ying Zhang ; Liliang Zhou ; Lingjing Xue ; xuelingjing65@163.com" class="auth_mail" title="E-mail the corresponding author ; Can Zhang ; zhangcan@cpu.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：EGFR/HER2 dual inhibitor ; Oxazolo[4 ; 5-g]quinazolin-2(1H)-one scaffold ; Antitumor proliferation ; Molecular docking ; SAR
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：14 September 2016
- 年：2016
- 卷：120
- 期：Complete
- 页码：26-36
- 全文大小：1139 K
文摘
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Novel EGFR/HER2 inhibitors of oxazolo[4,5-g]quinazolin-2(1H)-one were synthesized.
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Four compounds exhibited high inhibition against EGFR and HER2 kinase.
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Comp. 12f had high inhibition against A549 and SK-Br3 cell lines.
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Comp. 12f exhibited the lower toxicity against HELF cell than Lapatinib.
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Comp. 12f presented higher inhibition in vivo antitumor activity than Lapatinib.