Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors
文献类型：期刊论文
| 作者 | Liu, Qing1,3,4; Cai, Xiaoqing1,3; Yang, Dehua1,3 ; Chen, Yi2; Wang, Yafang2; Shao, Liming4; Wang, Ming-Wei1,2,3,4
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2017-09-01 |
| 卷号 | 25期号:17页码:4579-4594 |
| 关键词 | Methyltransferase inhibitor Cycloalkyl substituted analogue Natural product Sinefungin |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2017.06.032 |
| 文献子类 | Article |
| 英文摘要 | A series of cycloalkyl substituted analogues of the natural product sinefungin lacking the amino-acid moiety was designed and synthesized. Two stereoisomers (6-R and 6-S) were separated and their bioactivities examined against EHMT1/2. Of which, compound 14d showed an inhibitory activity against EHMT1/2 (88.9%, IC50 = 21.8 mu M for EHMT1 and 77.6%, IC50 = 39.6 mu M for EHMT2, respectively) similar to that of sinefungin (100.0%, IC50 = 28.4 mu M for EHMT1 and 79.5%, IC50 = 30.1 mu M for EHMT2, respectively). Further studies against other methyltransferases such as PRMT1 showed no activity except that 12d displayed about 20% inhibition. (C) 2017 Elsevier Ltd. All rights reserved. |
| WOS关键词 | HISTONE METHYLTRANSFERASE ; MODIFYING ENZYMES ; G9A ; GLP ; METHYLATION ; MECHANISM ; TARGETS |
| 资助项目 | National Health and Family Planning Commission of China[2012ZX09304-011] ; National Health and Family Planning Commission of China[2013ZX09401003-005] ; National Health and Family Planning Commission of China[2013ZX09507001] ; National Health and Family Planning Commission of China[2013ZX09507-002] ; National Health and Family Planning Commission of China[2014ZX09507002-001] ; National Natural Science Foundation of China[21302202] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Thousand Talents Program in China[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000407831300005 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272512]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Shao, Liming; Wang, Ming-Wei |
| 作者单位 | 1.Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 4.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Liu, Qing,Cai, Xiaoqing,Yang, Dehua,et al. Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2017,25(17):4579-4594. |
| APA | Liu, Qing.,Cai, Xiaoqing.,Yang, Dehua.,Chen, Yi.,Wang, Yafang.,...&Wang, Ming-Wei.(2017).Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,25(17),4579-4594. |
| MLA | Liu, Qing,et al."Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 25.17(2017):4579-4594. |
入库方式： OAI收割
来源：上海药物研究所
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