Design, Synthesis and Activities of Aziridine Derivatives of N^5-Methyltetrahydrofolate Against Methionine Synthase  

作　　者：DENG Xiling GUO Ying TIAN Chao LIU Junyi WANG Xiaowei ZHANG Zhili 

机构地区：[1]School of Pharmaceutical Sciences, 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

出　　处：《Chemical Research in Chinese Universities》2015年第5期742-745,共4页高等学校化学研究（英文版）

基　　金：Supported by the National Natural Science Foundation of China（No.21172014）.

摘　　要：Aziridine derivatives of N^5-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（IC55=24.42 μmol/L）. The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase.Aziridine derivatives of N^5-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（IC55=24.42 μmol/L）. The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase.

关 键 词：AZIRIDINE Methionine synthase Ring closure reaction N^5-Methyltetrahydrofolate 

分 类 号：O626.41[理学—有机化学] Q552[理学—化学]