Aziridine derivatives of N^5-methyltetrahydrofolate were designed and synthesized based on the mechanism of methionine synthase, and their biological activities were investigated as well. The aziridine derivatives 1 a...Aziridine derivatives of N^5-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（IC55=24.42 μmol/L）. The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase.展开更多
An efficient triethylamine-catalyzed synthesis of 4-amino-3,5-dicyano-6-arylphthalates is described.A one-pot,simple pseudo four-component reaction between arylaldehydes,dialkyl acetylenedicarboxylates, and twice as m...An efficient triethylamine-catalyzed synthesis of 4-amino-3,5-dicyano-6-arylphthalates is described.A one-pot,simple pseudo four-component reaction between arylaldehydes,dialkyl acetylenedicarboxylates, and twice as much malononitrile gave 4-amino-3,5-dicyano-6-arylphthalates in good to excellent yields.展开更多
基金Supported by the National Natural Science Foundation of China（No.21172014）.
文摘Aziridine derivatives of N^5-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（IC55=24.42 μmol/L）. The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase.
基金the financial support from the Research Council of Payame Noor University(PNU),Abhar-lran, and my colleague Ismail Hasani Asl
文摘An efficient triethylamine-catalyzed synthesis of 4-amino-3,5-dicyano-6-arylphthalates is described.A one-pot,simple pseudo four-component reaction between arylaldehydes,dialkyl acetylenedicarboxylates, and twice as much malononitrile gave 4-amino-3,5-dicyano-6-arylphthalates in good to excellent yields.
