Design, synthesis, and screen of cathepsin K inhibitors |
| |
| Authors: | Ying-Ying Yu Wei Sun Lei Dong Hai-Dong Liu Dan Jiang Jun-Hai Xiao Xiao-Hong Yang Song Li |
| |
| Institution: | a School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China;
b Laboratory of Computer-Aided Drug Design and Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China;
c First Affiliated Hospital of Jilin University, Changchun 130021, China |
| |
| Abstract: | We synthesized a series of epoxysuccinic acid derivatives and evaluated their in vitro cathepsin K inhibitory activity The screening results show that the potency of compounds 9e, 9d, 9p, 9j and 9k (IC50≤0.005 μmol/L) were equal to or greater than that of the lead compound 9a. Less hydrophobic compounds showed weaker potency, which can be explained by the hydrophobic nature of the cathepsin K binding pockets. |
| |
| Keywords: | Epoxysuccinic acid derivatives Synthesis Inhibitors Cathepsin K |
| 本文献已被 CNKI ScienceDirect 等数据库收录！ |
| 点击此处可从《中国化学快报》浏览原始摘要信息 |
| 点击此处可从《中国化学快报》下载免费的PDF全文 |
|
