Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells

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	Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells
其他题名	Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells
	Qin MingZe 1; Wang Lei 1; Yan Shuang 1; Ma JunJie 2; Tian Ye 1; Zhao YanFang 1; Gong Ping 1
	2017
发表期刊	CHINESE CHEMICAL LETTERS
ISSN	1001-8417
卷号	28 期号:5 页码:991-994
摘要	Based on our previous work, a series of hydrazone moiety-bearing aminopyrimidines were synthesized. The compounds were evaluated for inhibitory activities against EGFR T790M/L858R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR. Compounds 7f and 7k exhibited potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells (IC50; 0.45, 0.2 mu mol/L) while were much less active on A549 cancer cells (IC50; 52.83, >100 mu mol/L). Both compounds could be served as promising lead compounds for further investigation. (C) 2016 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
其他摘要	Based on our previous work, a series of hydrazone moiety-bearing aminopyrimidines were synthesized. The compounds were evaluated for inhibitory activities against EGFR T790M/L858R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR. Compounds 7f and 7k exhibited potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells (IC_(50); 0.45, 0.2 μmol/L) while were much less active on A549 cancer cells (IC_(50); 52.83, >100 μmol/L). Both compounds could be served as promising lead compounds for further investigation.
关键词	TYROSINE KINASE INHIBITOR LUNG-CANCER RECEPTOR T790M MUTANT MUTATION Aminopyrimidines EGFR T790M/L858R Selectivity Anti-resistance Antiproliferative activity
收录类别	CSCD
语种	英语
资助项目	[Science Foundation of Shenyang Pharmaceutical University]
CSCD记录号	CSCD:6017545
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/148169
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.华侨大学
推荐引用方式 GB/T 7714	Qin MingZe,Wang Lei,Yan Shuang,et al. Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells[J]. CHINESE CHEMICAL LETTERS,2017,28(5):991-994.
APA	Qin MingZe.,Wang Lei.,Yan Shuang.,Ma JunJie.,Tian Ye.,...&Gong Ping.(2017).Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells.CHINESE CHEMICAL LETTERS,28(5),991-994.
MLA	Qin MingZe,et al."Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells".CHINESE CHEMICAL LETTERS 28.5(2017):991-994.