Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors
文献类型：期刊论文
| 作者 | Shi, Ying1; Wu, Yan-Ran1; Su, Ming-Bo2; Shen, Dong-Hao1; Gunosewoyo, Hendra3; Yang, Fan1; Li, Jia2 ; Tang, Jie4; Zhou, Yu-Bo2; Yu, Li-Fang1
|
| 刊名 | RSC ADVANCES
 |
| 出版日期 | 2018 |
| 卷号 | 8期号:3页码:1666-1676 |
| ISSN号 | 2046-2069 |
| DOI | 10.1039/c7ra13097j |
| 文献子类 | Article |
| 英文摘要 | Herein we describe the design, synthesis, and biological evaluation of a novel series of tranylcypromine-based LSD1 inhibitors via conformational restriction using spiro ring systems. A simple, direct spirocyclic analog of tranylcypromine (compounds 8a and 8b) was shown to be a 28- to 129-fold more potent inhibitor of LSD1 enzyme compared to tranylcypromine. Further incorporation of various substituted benzyl groups to the amino group resulted in a suite of 2',3'-dihydrospiro[cyclopropane-1,1'-inden]-2-amines that are potent LSD1 inhibitors with excellent selectivity profiles (e.g. 14a, 15b, 16a, 19a and 20b) against closely related enzymes such as MAO-A, MAO-B, and LSD2. |
| WOS关键词 | HISTONE DEMETHYLASE ; CANCER-THERAPY ; POTENT ; LYSINE-SPECIFIC-DEMETHYLASE-1 ; PROLIFERATION ; METASTASIS ; SCAFFOLDS ; AGENTS |
| 资助项目 | Natural Science Foundation of Shanghai[16DZ2280100] ; Chinese Academy of Sciences[XDA12020313] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000419371200059 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272347]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Zhou, Yu-Bo; Yu, Li-Fang |
| 作者单位 | 1.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China; 3.Curtin Univ, Fac Hlth Sci, Sch Pharm, Bentley, WA 6102, Australia; 4.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Key Lab Green Chem & Chem Proc, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China |
| 推荐引用方式 GB/T 7714 | Shi, Ying,Wu, Yan-Ran,Su, Ming-Bo,et al. Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors[J]. RSC ADVANCES,2018,8(3):1666-1676. |
| APA | Shi, Ying.,Wu, Yan-Ran.,Su, Ming-Bo.,Shen, Dong-Hao.,Gunosewoyo, Hendra.,...&Yu, Li-Fang.(2018).Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors.RSC ADVANCES,8(3),1666-1676. |
| MLA | Shi, Ying,et al."Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors".RSC ADVANCES 8.3(2018):1666-1676. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。