Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors
文献类型：期刊论文
| 作者 | Xie, Yunfeng3; Chen, Xianjie1; Qin, Jie4; Kong, Xiangqian2; Ye, Fei2; Jiang, Yuren3; Liu, Hong2 ; Jiang, Hualiang1,2; Marmorstein, Ronen4; Luo, Cheng2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2013-04-15 |
| 卷号 | 23期号:8页码:2306-2312 |
| 关键词 | BRAF Kinase inhibitors Virtual screening Anticancer agents |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2013.02.072 |
| 文献子类 | Article |
| 英文摘要 | The V600E BRAF kinase mutation, which activates the downstream MAPK signaling pathway, commonly occurs in about 8% of all human malignancies and about 50% of all melanomas. In this study, we employed virtual screening and chemical synthesis to identify a series of N-(thiophen-2-yl) benzamide derivatives as potent BRAF(V600E) inhibitors. Structure-activity relationship studies of these derivatives revealed that compounds b40 and b47 are the two most potent BRAFV600E inhibitors in this series. (C) 2013 Elsevier Ltd. All rights reserved. |
| WOS关键词 | B-RAF INHIBITORS ; B-RAF(V600E) INHIBITORS ; BRAF INHIBITORS ; MUTANT BRAF ; KINASE ; RESISTANCE ; MELANOMA ; OPTIMIZATION ; DISCOVERY ; DOCKING |
| 资助项目 | National Natural Science Foundation of China[20972174] ; National Natural Science Foundation of China[91029704] ; National Natural Science Foundation of China[21210003] ; National Natural Science Foundation of China[21021063] ; State Key Program of Basic Research of China[2009CB918502] ; 863 program[2012AA020302] ; National Science and Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2013ZX09507-004] ; National Institutes of Health[CA114046] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000316934000006 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277653]  |
| 专题 | 药物发现与设计中心 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 | Jiang, Yuren |
| 作者单位 | 1.Nanjing Univ, Nanjing Natl Lab Microstruct, Sch Chem & Chem Engn, Nanjing 210093, Jiangsu, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Cent S Univ, Coll Chem & Chem Engn, Changsha 410083, Peoples R China; 4.Wistar Inst Anat & Biol, Philadelphia, PA 19104 USA; |
| 推荐引用方式 GB/T 7714 | Xie, Yunfeng,Chen, Xianjie,Qin, Jie,et al. Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(8):2306-2312. |
| APA | Xie, Yunfeng.,Chen, Xianjie.,Qin, Jie.,Kong, Xiangqian.,Ye, Fei.,...&Luo, Cheng.(2013).Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(8),2306-2312. |
| MLA | Xie, Yunfeng,et al."Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.8(2013):2306-2312. |
入库方式： OAI收割
来源：上海药物研究所
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