Semisynthesis of ent-norstrobane diterpenoids as potential inhibitor for factor Xa |
| |
| Authors: | Jianbin Wang He Ma Hongzheng Fu |
| |
| Institution: | 1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Science, Peking University, Beijing 100191, People’s Republic of China;2. Guangdong-Macau Traditional Chinese Medicine Technology Industrial Park Development Co., Ltd., Zhuhai 519000, People’s Republic of China;3. Shandong Academy of Pharmaceutical Sciences, Jinan 250101, People’s Republic of China |
| |
| Abstract: | A semisynthesis of two ent-strobane diterpenoids strobols C (7) and D (14) was accomplished via a Wagnar-Meerwein rearrangement. Compounds 7, 14, and the intermediate products were evaluated for their inhibition on factor Xa (FXa). Among all the compounds screened for FXa inhibitory activity, three compounds 6, 7, and 9 showed significant inhibitory activities with IC50 values of 1067?±?164, 81?±?11, 1023?±?89?nM, respectively. The inhibitory activity on FXa described in this study highlight the importance of structural modification based on natural products in the development of FXa inhibitors. |
| |
| Keywords: | Semisynthesis Wagnar-Meerwein rearrangement Factor Xa |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
