|
|||||
|
|
Design,Synthesis and Activities of Aziridine Derivatives of N5-Methyltetrahydrofolate Against Methionine Synthase |
|
| Authors: | DENG Xiling GUO Ying TIAN Chao LIU Junyi WANG Xiaowei ZHANG Zhili |
| Affiliation: | 1. School of Pharmaceutical Sciences, Peking University, Beijing 100191, P. R. China; 2. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, P. R. China; 3. School of Pharmaceutical Sciences, Shihezi University, Shihezi 832000, P. R. China |
| Abstract: | Aziridine derivatives of N5-methyltetrahydrofolate were designed and synthesized based on the mechanism of methionine synthase, and their biological activities were investigated as well. The aziridine derivatives 1 and 6 exhibited superior inhibitory activities(IC50: 5.05 and 4.15 μmol/L, respectively) compared to the corresponding chain analogue 4(IC50=24.42 μmol/L). The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase. |
| Keywords: | Aziridine Methionine synthase Ring closure reaction N5-Methyltetrahydrofolate |
| 本文献已被 万方数据 等数据库收录！ | |
| 点击此处可从《高等学校化学研究》浏览原始摘要信息 | |
| 点击此处可从《高等学校化学研究》下载全文 | |