Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors
文献类型：期刊论文
| 作者 | Mao, Yongjun1; Zhu, Wenxiu2; Kong, Xiaoguang2; Wang, Zhen1 ; Xie, Hua1; Ding, Jian1; Terrett, Nicholas Kenneth2; Shen, Jingkang1; Shen, Jingshan1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2013-06-01 |
| 卷号 | 21期号:11页码:3090-3104 |
| 关键词 | EGFR 5-Ethynylpyrimidine 4-Anilino-3-cyano-5-phenylpyridine m-Amino-N-phenylbenzamide Tyrosine kinase inhibitors |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2013.03.053 |
| 文献子类 | Article |
| 英文摘要 | 36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from the bioactivity and chemical structures yield preliminary structure-activity relationships (SARs). The most potent 5-ethynylpyrimidine derivative 20a has an IC50 value of 45 nM to EGFR kinase. Several compounds of other series also show IC50 values <1 mu M for EGFR and <5 mu M for A-549 and HL60 cells growth inhibition. (C) 2013 Published by Elsevier Ltd. |
| WOS关键词 | DUAL INHIBITORS ; ERBB RECEPTORS ; GROWTH ; CANCER ; HER-2 ; OPTIMIZATION ; SERIES ; DISCOVERY |
| 资助项目 | National High Technology Research and Development Program of China[2012AA020302] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000319002600029 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277603]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Shen, Jingshan |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Vitargeta Therapeut Inc, Plainsboro, NJ 08536 USA |
| 推荐引用方式 GB/T 7714 | Mao, Yongjun,Zhu, Wenxiu,Kong, Xiaoguang,et al. Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2013,21(11):3090-3104. |
| APA | Mao, Yongjun.,Zhu, Wenxiu.,Kong, Xiaoguang.,Wang, Zhen.,Xie, Hua.,...&Shen, Jingshan.(2013).Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,21(11),3090-3104. |
| MLA | Mao, Yongjun,et al."Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 21.11(2013):3090-3104. |
入库方式： OAI收割
来源：上海药物研究所
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