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Design, synthesis and activities of aziridine derivatives of N5-methyltetrahydrofolate against methionine synthase

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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.

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Correspondence to Zhili Zhang.

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

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Deng, X., Guo, Y., Tian, C. et al. Design, synthesis and activities of aziridine derivatives of N5-methyltetrahydrofolate against methionine synthase. Chem. Res. Chin. Univ. 31, 742–745 (2015). https://doi.org/10.1007/s40242-015-5194-z

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  • DOI: https://doi.org/10.1007/s40242-015-5194-z

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