高等学校化学研究 ›› 2015, Vol. 31 ›› Issue (5): 742-745.doi: 10.1007/s40242-015-5194-z
Design, Synthesis and Activities of Aziridine Derivatives of N5-Methyltetrahydrofolate Against Methionine Synthase
DENG Xiling1,3, GUO Ying1, TIAN Chao1, LIU Junyi1,2, WANG Xiaowei1, ZHANG Zhili1
- 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
Design, Synthesis and Activities of Aziridine Derivatives of N5-Methyltetrahydrofolate Against Methionine Synthase
DENG Xiling1,3, GUO Ying1, TIAN Chao1, LIU Junyi1,2, WANG Xiaowei1, ZHANG Zhili1
- 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
摘要：
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.