Design, synthesis, and SAR of embelin analogues as the inhibitors of PAI-1 (plasminogen activator inhibitor-1)
文献类型：期刊论文
| 作者 | Chen, Fanglei2; Zhang, Guiping2; Hong, Zebin1; Lin, Zhonghui1; Lei, Min2 ; Huang, Mingdong1; Hu, Lihong2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2014-05-15 |
| 卷号 | 24期号:10页码:2379-2382 |
| 关键词 | Embelin Natural product PAI-1 Inhibitory activity SAR study |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2014.03.045 |
| 文献子类 | Article |
| 英文摘要 | The natural product embelin was found to have PAI-1 inhibitory activity with the IC50 value of 4.94 mu M. Based on the structure of embelin, a series of analogues were designed, synthesized, and evaluated for their ability to inhibit PAI-1. The SAR study on these compounds disclosed that the inhibitory potency largely depended on the hydroxyl groups at C2 and C5, and the length of the alkyl chains at C3 and C6. Compound 11 displayed the best PAI-1 inhibitory potency with the IC50 value of 0.18 mu M. (C) 2014 Elsevier Ltd. All rights reserved. |
| WOS关键词 | BREAST-CANCER PATIENTS ; MYOCARDIAL-INFARCTION ; VENOUS THROMBOSIS ; INDUCED APOPTOSIS ; PLASMA-LEVELS ; IN-VITRO ; DERIVATIVES ; SYSTEM ; CELLS ; RISK |
| 资助项目 | National Natural Science Foundation of China[30925040] ; National Natural Science Foundation of China[81102329] ; National Natural Science Foundation of China[81273397] ; Chinese National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2013ZX09508104] ; Science Foundation of Shanghai[12XD1405700] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000335517300029 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277076]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Huang, Mingdong |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Struct Chem, Fujian Inst Res Struct Matter, Fuzhou 350002, Peoples R China 2.Chinese Acad Sci, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Chen, Fanglei,Zhang, Guiping,Hong, Zebin,et al. Design, synthesis, and SAR of embelin analogues as the inhibitors of PAI-1 (plasminogen activator inhibitor-1)[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2014,24(10):2379-2382. |
| APA | Chen, Fanglei.,Zhang, Guiping.,Hong, Zebin.,Lin, Zhonghui.,Lei, Min.,...&Hu, Lihong.(2014).Design, synthesis, and SAR of embelin analogues as the inhibitors of PAI-1 (plasminogen activator inhibitor-1).BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,24(10),2379-2382. |
| MLA | Chen, Fanglei,et al."Design, synthesis, and SAR of embelin analogues as the inhibitors of PAI-1 (plasminogen activator inhibitor-1)".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 24.10(2014):2379-2382. |
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。