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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