Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors
文献类型：期刊论文
| 作者 | Yang, Wei2; Li, Lixuan1,3; Wang, Yulan1; Wu, Xiaowei2; Li, Tingting; Yang, Nan ; Su, Mingbo1; Sheng, Li1; Zheng, Mingyue1; Zang, Yi1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-09-01 |
| 卷号 | 23期号:17页码:5881-5890 |
| 关键词 | HDACs HDACs inhibitor Hydroxamic acid Isoquinoline |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2015.06.071 |
| 文献子类 | Article |
| 英文摘要 | The design, synthesis and biological evaluation of a series of isoquinoline-based hydroxamic acid compounds as novel HDACs inhibitors were reported herein. A detailed SAR study showed most of the compounds displayed good to excellent inhibitory activities against HDAC1, 3, 6. The IC50 values of compound 10c against HDAC1, 3, 6 were 4.17 +/- 0.11 nM, 4.00 +/- 0.10 nM, 3.77 +/- 0.07 nM, respectively. Most of the compounds showed great anti-proliferative activities against RPMI 8226, HCT 116 and Hep G2 cells. The IC50 values of compounds 10a-h against RPMI 8226 cancer cell proliferation were all below 1 mu M. HCT 116 cell was sensitive to the compounds 10a, 10f-g and 18a with the IC50 values <0.3 mu M. The active compounds 10a-d did not show inhibitory activity against hERG channel. All these evidence indicated these compounds had great potential as HDACs inhibitors for the further development. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | HDAC INHIBITORS ; THERAPY ; CANCER ; SAHA ; DEPSIPEPTIDE ; ACETYLATION ; DISEASES ; AGENT |
| 资助项目 | National Natural Science Foundation of China[21021063] ; National Natural Science Foundation of China[91229204] ; National Natural Science Foundation of China[81125023] ; National Natural Science Foundation of China[81173033] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103101-072] ; National S&T Major Projects[2012ZX09301001-005] ; National S&T Major Projects[2013ZX09507-001] ; Chinese Academy of Science 'strategic leader in science and technology projects'[XDA01040303] ; Program of Shanghai Subject Chief Scientist[12XD1407100] ; Program of Shanghai Subject Chief Scientist[13XD1404300] ; National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program' of China[2014ZX09507-002] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000360349900067 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276422]  |
| 专题 | 国家新药筛选中心 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 药物安全性评价中心 |
| 通讯作者 | Li, Jia |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 3.E China Normal Univ, Inst Adv Interdisciplinary Res, Shanghai 200062, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Wei,Li, Lixuan,Wang, Yulan,et al. Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(17):5881-5890. |
| APA | Yang, Wei.,Li, Lixuan.,Wang, Yulan.,Wu, Xiaowei.,Li, Tingting.,...&Liu, Hong.(2015).Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,23(17),5881-5890. |
| MLA | Yang, Wei,et al."Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 23.17(2015):5881-5890. |
入库方式： OAI收割
来源：上海药物研究所
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