河北师范大学学报—

期刊信息

刊名：河北师范大学学报（自然科学版）Journal of Hebei Normal University (Natural Science)
主办：河北师范大学
ISSN： 1000-5854
CN： 13-1061/N
中国科技核心期刊
中国期刊方阵入选期刊
中国高校优秀科技期刊
华北优秀期刊
河北省优秀科技期刊

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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

李英俊¹

曹欣¹

高立信²

靳焜³

李继阳¹

盛丽²

李佳²

1. 辽宁师范大学化学化工学院, 辽宁大连 116029;
2. 中国科学院上海药物研究所, 国家新药筛选中心, 药物研究国家重点实验室, 上海 201203;
3. 大连理工大学精细化工国家重点实验室, 辽宁大连 116012
DOI： 10.13763/j.cnki.jhebnu.nse.2017.02.009

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

LI Yingjun¹, CAO Xin¹, GAO Lixin², JIN Kun³, LI Jiyang¹, SHENG Li², LI Jia²

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摘要/Abstract

摘要：

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.

Abstract：

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 ¹H NMR 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.

关键词

关键词： 酰腙 ; 苯并咪唑 ; 合成 ; Cdc25B和PTP1B ; 抑制活性

Key words： acylhydrazone ; benzimidazole ; synthesis ; Cdc25B and PTP1B ; inhibitory activity

参考文献 19

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