Design,Synthesis and Activities of Aziridine Derivatives of N5-Methyltetrahydrofolate Against Methionine Synthase期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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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

Institution:	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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