| 3,6-二取代三唑并噻二唑衍生物的合成及其对细胞分裂周期25B磷酸酶和蛋白酪氨酸磷酸酶1B抑制活性评价 |
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| 引用本文： | 李英俊,杨鸿境,曹欣,高立信,靳焜,盛丽,刘季红,刘雪洁,李佳. 3,6-二取代三唑并噻二唑衍生物的合成及其对细胞分裂周期25B磷酸酶和蛋白酪氨酸磷酸酶1B抑制活性评价[J]. 应用化学, 2020, 37(9): 994-1002. DOI: 10.11944/j.issn.1000-0518.2020.09.200040 |
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| 作者姓名： | 李英俊 杨鸿境 曹欣 高立信 靳焜 盛丽 刘季红 刘雪洁 李佳 |
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| 作者单位： | 辽宁师范大学化学化工学院 辽宁 大连 116029;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;大连理工大学精细化工国家重点实验室 辽宁 大连 116012;大连理工大学化学分析测试中心 辽宁 大连 116023 |
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| 基金项目： | 辽宁省自然科学基金(20102126)项目资助 |
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| 摘 要： | 合成出了一系列含苯并咪唑/芳氧甲基骨架的3,6-二取代三唑并噻二唑衍生物3a~3l,其结构经傅里叶变换红外光谱仪(FT-IR)、核磁共振波谱仪(NMR)和元素分析得以确认。 评价了它们对细胞分裂周期25B磷酸酶(Cdc25B)/蛋白酪氨酸磷酸酶1B(PTP1B)的抑制活性,讨论了构效关系。 生物活性测试结果显示,化合物3a对Cdc25B和PTP1B的抑制活性最高,其半数抑制浓度(IC50)值分别为(0.46±0.02) μg/mL和(1.77±0.40) μg/mL。 所得研究结果为开发新型Cdc25B/PTP1B抑制剂提供了参考依据。
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| 关 键 词： | 三唑并噻二唑 苯并咪唑 芳氧乙酸 细胞分裂周期25B磷酸酶抑制剂 蛋白酪氨酸磷酸酶1B抑制剂 |
| 收稿时间： | 2020-02-16 |
Synthesis of 3,6-Disubstituted Triazolothiadiazole Derivatives and Their Inhibitory Activities Against Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B |
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| LI Yingjun,YANG Hongjing,CAO Xin,GAO Lixin,JIN Kun,SHENG Li,LIU Jihong,LIU Xuejie,LI Jia. Synthesis of 3,6-Disubstituted Triazolothiadiazole Derivatives and Their Inhibitory Activities Against Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B[J]. Chinese Journal of Applied Chemistry, 2020, 37(9): 994-1002. DOI: 10.11944/j.issn.1000-0518.2020.09.200040 |
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| Authors: | LI Yingjun YANG Hongjing CAO Xin GAO Lixin JIN Kun SHENG Li LIU Jihong LIU Xuejie LI Jia |
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| Affiliation: | College of Chemistry and Chemical Engineering,Liaoning Normal University,Dalian,Liaoning 116029,China;National Center for Drug Screening,State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China;State Key Laboratory of Fine Chemicals,Dalian University of Technology,Dalian,Liaoning 116012,China;Chemistry Analysis and Inspection Center,Dalian University of Technology,Dalian,Liaoning 116023,China |
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| Abstract: | A series of 3,6-disubstituted triazolothiadiazole derivatives 3a-3l containing benzimidazole/aryloxymethyl scaffolds was synthesized. Their structures were confirmed by Fourier transform infrared spectrometry (FT-IR), nuclear magnetic resonance spectroscopy (NMR) and elemental analysis. The inhibitory activity of all synthesized target compounds against cell division cycle 25B phosphatase (Cdc25B)/protein tyrosine phosphatase 1B (PTP1B) was evaluated, and the structure-activity relationship was discussed. The bioassay results show that target compound 3a has the highest inhibitory activity against Cdc25B and PTP1B with the half inhibitory concentration (IC50) values of (0.46±0.02) μg/mL and (1.77±0.40) μg/mL, respectively. The obtained research results provide a reference for the development of novel Cdc25B/PTP1B inhibitors. |
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| Keywords: | triazolothiadiazole benzimidazole aryloxyacetic acid cell division cycle 25B phosphatase inhibitor protein tyrosine phosphatase 1B inhibitor |
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