Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy
文献类型：期刊论文
| 作者 | Gong, Chao-Jun; Gao, An-Hui; Zhang, Yang-Ming ; Su, Ming-Bo; Chen, Fei; Sheng, Li; Zhou, Yu-Bo; Li, Jing-Ya; Li, Jia; Nan, Fa-Jun
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2016-04-13 |
| 卷号 | 112页码:81-90 |
| 关键词 | Bisthiazole Histone deacetylases ZBG Trifluoromethyl ketones |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2016.02.003 |
| 文献子类 | Article |
| 英文摘要 | Histone deacetylases (HDACs) are a class of epigenetic modulators with complex functions in histone post-translational modifications and are well known targets for antineoplastic drugs. We have previously developed a series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors. In the present work, a new series of bisthiazole-based compounds with different zinc binding groups (ZBGs) have been designed and synthesized. Among them is compound 7, containing a trifluoromethyl ketone as the ZBG, which displays potent inhibitory activity towards human HDACs and improved antiproliferative activity in several cancer cell lines. (C) 2016 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | HISTONE DEACETYLASE INHIBITION ; LYMPHOMA ; APPROVAL ; MYELOMA ; CANCER ; LBH589 |
| 资助项目 | National Natural Science Foundation of China[81321092] ; Science and Technology Commission of Shanghai Municipality[14431906100] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000372558200008 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276076]  |
| 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 药物安全性评价中心 |
| 通讯作者 | Li, Jia; Nan, Fa-Jun |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Chinese Natl Ctr Drug Screening, 189 Guoshoujing Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Gong, Chao-Jun,Gao, An-Hui,Zhang, Yang-Ming,et al. Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,112:81-90. |
| APA | Gong, Chao-Jun.,Gao, An-Hui.,Zhang, Yang-Ming.,Su, Ming-Bo.,Chen, Fei.,...&Nan, Fa-Jun.(2016).Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,112,81-90. |
| MLA | Gong, Chao-Jun,et al."Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 112(2016):81-90. |
入库方式： OAI收割
来源：上海药物研究所
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