含苯并咪唑环N-酰腙衍生物的合成及作为Cdc25B和PTP1B抑制剂的生物评价

Synthesis and Biological Evaluation of N-acylhydrazone Derivatives Containing Benzimidazole Moiety as Cdc25B and PTP1B Inhibitors

以酚和氯乙酸为起始原料,经多步反应,合成出了14个新型的含苯并咪唑环N-酰腙衍生物5a^5n,并利用IR,~1HNMR和元素分析确定了其结构.评价了目标化合物对Cdc25B和PTP1B的抑制活性,讨论了结构与活性的关系.实验结果表明,大部分化合物对PTP1B显示出良好的抑制活性(IC50=(6.43±0.88)^(19.76±4.00)μg/mL),其中5h的抑制活性最高(IC50=(6.43±0.88)μg/mL).目标化合物5a^5n对Cdc25B有弱的抑制活性.

Fourteen new N-acylhydrazone derivatives containing benzimidazole moiety 5a-5n were synthesized by substituted phenol and chloroacetic acid as starting materials via multistep reactions. Their structures were confirmed by elemental analysis, IR and 1HNMR spectra. The synthesized target compounds 5 were evaluated for the inhibitory activities against Cdc25B and PTP1B. The structure-activity relationship was also discussed. The experimental results showed that most compounds exhibited good inhibitory activities against PTP1B （IC50 = （6.43±0.88）-（19.76±4.00） μg/mL）. Among of them,compound 5h exhibited highest inhibitory activity （IC50=（6.43± 0.88） μg/mL）. The target compounds 5a-5n had weak inhibitory activity for Cdc25B.