Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors
文献类型：期刊论文
| 作者 | Ji, Xun1,3; Peng, Ting2; Zhang, Xu1; Li, Jian1; Yang, Wei1; Tong, Linjiang2; Qu, Rong2; Jiang, Hualiang1,3 ; Ding, Jian2; Xie, Hua2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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| 出版日期 | 2014-04-01 |
| 卷号 | 22期号:7页码:2366-2378 |
| ISSN号 | 0968-0896 |
| 关键词 | Irreversible EGFR inhibitor EGFR T790M/L858R Thieno[2,3-d]pyrimidines |
| DOI | 10.1016/j.bmc.2014.01.035 |
| 文献子类 | Article |
| 英文摘要 | A novel series of 6-alkenylamides of 4-anilinothieno[2,3-d]pyrimidine derivatives was designed, synthesized and evaluated as irreversible inhibitors of the epidermal growth factor receptor (EGFR). Most of the compounds exhibited good potency against EGFR wild type (EGFR wt) and EGFR T790M/L858R. Among these, the half-maximal inhibitory concentration (IC50) values of 17 compounds against EGFR wt were less than 0.020 mu M, and those of 12 compounds were less than 0.010 mu M. The IC50 values of 10 compounds against EGFR T790M/L858R were less than 0.005 mu M. Compounds 8l, 9n, 9o, 9q and 9v almost completely blocked the phosphorylation of EGFR in the A431 cell line at 1 mu M. Compounds 8l, 9n, 9o, 9q and 9v blocked the autophosphorylation of EGFR in NCI-H1975 cells at high concentration (1 mu M), and compound 8l was confirmed to be an irreversible inhibitor through the dilution method. (c) 2014 Published by Elsevier Ltd. |
| WOS关键词 | TYROSINE KINASE INHIBITORS ; BETA-AMINO ACIDS ; FLUORINE-CONTAINING AMINES ; CELL LUNG-CANCER ; ASYMMETRIC-SYNTHESIS ; EGFR ; RESISTANCE ; OPTIMIZATION ; DERIVATIVES ; BEARING |
| 资助项目 | National Natural Science Foundation of China[21021063] ; National Natural Science Foundation of China[91229204] ; National Natural Science Foundation of China[81025017] ; National Natural Science Foundation of China[81173080] ; National S&T Major Projects[2012ZX09103101-072] ; National S&T Major Projects[2012ZX09301001-005] ; National S&T Major Projects[2013ZX09507-001] ; Program of Shanghai Subject Chief Scientist[12XD1407100] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000334337800037 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277135]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 |
| 通讯作者 | Xie, Hua |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Liaoning, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ji, Xun,Peng, Ting,Zhang, Xu,et al. Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2014,22(7):2366-2378. |
| APA | Ji, Xun.,Peng, Ting.,Zhang, Xu.,Li, Jian.,Yang, Wei.,...&Liu, Hong.(2014).Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,22(7),2366-2378. |
| MLA | Ji, Xun,et al."Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 22.7(2014):2366-2378. |
入库方式： OAI收割
来源：上海药物研究所
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