| Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells | |
| Alternative Title | Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells |
| Qin MingZe1; Wang Lei1; Yan Shuang1; Ma JunJie2; Tian Ye1; Zhao YanFang1; Gong Ping1 | |
| 2017 | |
| Source Publication | CHINESE CHEMICAL LETTERS
 |
| ISSN | 1001-8417 |
| Volume | 28Issue:5Pages:991-994 |
| Abstract | 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. |
| Other Abstract | 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. |
| Keyword | TYROSINE KINASE INHIBITOR LUNG-CANCER RECEPTOR T790M MUTANT MUTATION Aminopyrimidines EGFR T790M/L858R Selectivity Anti-resistance Antiproliferative activity |
| Indexed By | CSCD |
| Language | 英语 |
| Funding Project | [Science Foundation of Shenyang Pharmaceutical University] |
| CSCD ID | CSCD:6017545 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.imr.ac.cn/handle/321006/148172 |
| Collection | 中国科学院金属研究所 |
| Affiliation | 1.中国科学院金属研究所 2.华侨大学 |
| Recommended Citation 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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