Design, synthesis and evaluation of a novel BRD4 protein inhibitors
文献类型：期刊论文
| 作者 | Hu Jianping; Li Yanlian; Shi Huanyu; Xiong Bing ; Shen Jingkang
|
| 刊名 | Acta Pharmaceutica Sinica
 |
| 出版日期 | 2017 |
| 卷号 | 52期号:10页码:1568-1577 |
| 关键词 | BRD4 BRD4 dihydroquinoxalin-2(1H)-one phenyl side chain |
| ISSN号 | 0513-4870 |
| 其他题名 | BRD4小分子抑制剂的设计、合成以及初步活性研究 |
| 文献子类 | Article |
| 英文摘要 | Bromodomain-containing proteins (BCPs) can specifically recognize acetylated lysine (KAc) in histones and other substrate proteins. Recently, several kinase inhibitors were found to inhibit bromodomains, such as the PLK1 inhibitor BI-2536 and the JAK2 inhibitor TG101209, which bind to BRD4 with IC_(50) values of 25 nmol·L~(-1) and 130 nmol·L~(-1), respectively. To obtain potent BRD4 inhibitors from inhibitor BI-2536, we used dihydroquinoxalin-2(1H)-one to replace the 7,8-dihydropteridin-6(5H)-one in BI2536. By exploring the structure-activity relationships of the new dihydroquinoxalin-2(1H)-one structures, we obtained a novel phenyl side chain series of BRD4 inhibitors. We identified several potent BRD4 inhibitors, especially compounds 16, 22, 28 and 29, which had IC_(50) values below 100 nmol·L~(-1) in fluorescence anisotropy (FA) assays, indicating this series of compounds are worth to fruther investigation. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:6078473 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269195]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Xiong Bing |
| 作者单位 | Department of Medicinal Chemistry, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China. |
| 推荐引用方式 GB/T 7714 | Hu Jianping,Li Yanlian,Shi Huanyu,et al. Design, synthesis and evaluation of a novel BRD4 protein inhibitors[J]. Acta Pharmaceutica Sinica,2017,52(10):1568-1577. |
| APA | Hu Jianping,Li Yanlian,Shi Huanyu,Xiong Bing,&Shen Jingkang.(2017).Design, synthesis and evaluation of a novel BRD4 protein inhibitors.Acta Pharmaceutica Sinica,52(10),1568-1577. |
| MLA | Hu Jianping,et al."Design, synthesis and evaluation of a novel BRD4 protein inhibitors".Acta Pharmaceutica Sinica 52.10(2017):1568-1577. |
入库方式： OAI收割
来源：上海药物研究所
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