Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells | |
Qin MingZe2; Wang Lei2; Yan Shuang2; Ma JunJie1; Tian Ye2; Zhao YanFang2; Gong Ping2 | |
刊名 | CHINESE CHEMICAL LETTERS
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2017 | |
卷号 | 28期号:5页码:991-994 |
关键词 | TYROSINE KINASE INHIBITOR LUNG-CANCER RECEPTOR T790M MUTANT MUTATION Aminopyrimidines EGFR T790M/L858R Selectivity Anti-resistance Antiproliferative activity |
ISSN号 | 1001-8417 |
其他题名 | Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells |
英文摘要 | 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. |
资助项目 | [Science Foundation of Shenyang Pharmaceutical University] |
语种 | 英语 |
CSCD记录号 | CSCD:6017545 |
内容类型 | 期刊论文 |
源URL | [http://ir.imr.ac.cn/handle/321006/148171] ![]() |
专题 | 金属研究所_中国科学院金属研究所 |
作者单位 | 1.华侨大学 2.中国科学院金属研究所 |
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. |
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