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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  
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