Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors
文献类型：期刊论文
| 作者 | Yu, Jianjun3; Xu, Lei1,2,4; Hong, Duidui3; Zhang, Xiaotuan1,2; Liu, Jieyu1,2; Li, Daqiang3; Li, Jia1,2 ; Zhou, Yubo1,2; Liu, Tao3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2019 |
| 卷号 | 161页码:543-558 |
| 关键词 | Proteasome inhibitor Non-covalent Non-peptide Phenol ether Solid cancers |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2018.10.056 |
| 文献子类 | Article |
| 英文摘要 | A series of novel phenol ether derivatives were designed, synthesized, and evaluated as non-covalent proteasome inhibitors. Most compounds exhibited moderate to excellent proteasome inhibitory activity. In particular, compound 18x proved to be the most potent compound (chymotrypsin-like: IC50 = 49 nM), exhibiting a 2-fold higher potency compared to the reported PI-1840. Besides, compound 18x exhibited excellent metabolic stability and selective anti-proliferative activity against solid cancer cell lines including HepG2 and HGC27, providing incentive for the further development as a potential anticancer agent against solid cancers. (C) 2018 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | CHYMOTRYPSIN-LIKE ACTIVITY ; 20S PROTEASOME ; IMMUNOPROTEASOME ; OPTIMIZATION ; PROTEOLYSIS ; DISCOVERY ; DOCKING ; POTENT ; SERIES |
| 资助项目 | key project of Zhejiang Provincial Natural Science Foundation of China[LZ15H300001] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000451498200038 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279462]  |
| 专题 | 新药研究国家重点实验室 国家新药筛选中心 |
| 通讯作者 | Zhou, Yubo; Liu, Tao |
| 作者单位 | 1.Univ Chinese Acad Sci, Grad Sch, 19A Yuquan Rd, Beijing 100049, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 3.Zhejiang Univ, ZJU ENS Joint Lab Med Chem, Zhejiang Prov Key Lab Anticanc Drug Res, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; 4.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yu, Jianjun,Xu, Lei,Hong, Duidui,et al. Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2019,161:543-558. |
| APA | Yu, Jianjun.,Xu, Lei.,Hong, Duidui.,Zhang, Xiaotuan.,Liu, Jieyu.,...&Liu, Tao.(2019).Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,161,543-558. |
| MLA | Yu, Jianjun,et al."Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 161(2019):543-558. |
入库方式： OAI收割
来源：上海药物研究所
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