Discovery of novel selective inhibitors for EGFR-T790M/L858R
文献类型：期刊论文
| 作者 | Bai, Fang1,2; Liu, Hongyan3; Tong, Linjiang3; Zhou, Wei4,5; Liu, Li4,5; Zhao, Zhenjiang4,5; Liu, Xiaofeng4,5; Jiang, Hualiang4,5,6 ; Wang, Xicheng1; Xie, Hua3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2012-02-01 |
| 卷号 | 22期号:3页码:1365-1370 |
| 关键词 | EGFR T790M/L858R Virtual screening Kinase inhibitors Selective inhibitors Dual-effective inhibitors |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2011.12.067 |
| 文献子类 | Article |
| 英文摘要 | Through a receptor-based and ligand-based combined virtual screening protocol, 21 novel compounds covering 15 scaffolds were identified as novel inhibitors for EGFR-T790M/L858R, among which, 12 of them were identified as selective inhibitors for EGFR-T790M/L858R to wild-type EGFR, and 5 of them exhibited 'dual-effective' to wild-type and mutant EGFR. Meanwhile, their antiproliferative effects toward EGFR high-expressing human lung cancer cell (A549), epidermoid carcinoma cell (A431), and the mutant EGFR-dependent cell (NCI-H1975) were also evaluated. (C) 2011 Elsevier Ltd. All rights reserved. |
| WOS关键词 | TYROSINE-KINASE INHIBITORS ; GROWTH-FACTOR RECEPTOR ; CELL LUNG-CANCER ; HYBRID APPROACH ; T790M MUTATION ; EGFR T790M ; RESISTANCE ; THERAPY ; CONFORMATION ; GEFITINIB |
| 资助项目 | Fundamental Research Funds for the Central Universities[00000000] ; National Natural Science Foundation of China[20803022 21173076] ; National Natural Science Foundation of China[81102375] ; Special Fund for Major State Basic Research Project[2009CB918501] ; Shanghai Committee of Science and Technology[09dZ1975700] ; Shanghai Committee of Science and Technology[10431902600] ; National S&T Major Project of China[2011ZX09307-002-03] ; Shanghai Rising-Star Program[10QA1401800] ; Program for New Century Excellent Talents in University[NCET-10-0378] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000300404200014 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278195]  |
| 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 药物发现与设计中心 |
| 通讯作者 | Wang, Xicheng |
| 作者单位 | 1.Dalian Univ Technol, Dept Engn Mech, State Key Lab Struct Anal Ind Equipment, Dalian 116023, Peoples R China; 2.Dalian Univ Technol, Fac Chem Environm & Biol Sci & Technol, Dalian 116023, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 4.E China Univ Sci & Technol, Sch Pharm, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China; 5.E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China; 6.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Bai, Fang,Liu, Hongyan,Tong, Linjiang,et al. Discovery of novel selective inhibitors for EGFR-T790M/L858R[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(3):1365-1370. |
| APA | Bai, Fang.,Liu, Hongyan.,Tong, Linjiang.,Zhou, Wei.,Liu, Li.,...&Li, Honglin.(2012).Discovery of novel selective inhibitors for EGFR-T790M/L858R.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(3),1365-1370. |
| MLA | Bai, Fang,et al."Discovery of novel selective inhibitors for EGFR-T790M/L858R".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.3(2012):1365-1370. |
入库方式： OAI收割
来源：上海药物研究所
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