| 吡咯并嘧啶类化合物的合成及其抑制JAK3激酶活性的研究 |
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| 引用本文： | 支爽,杨妙,商倩,陶遵威,刘登科. 吡咯并嘧啶类化合物的合成及其抑制JAK3激酶活性的研究[J]. 现代药物与临床, 2017, 32(4): 557-561. DOI: 10.7501/j.issn.1674-5515.2017.04.002 |
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| 作者姓名： | 支爽 杨妙 商倩 陶遵威 刘登科 |
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| 作者单位： | 1. 天津市医药科学研究所,天津 300020;天津大学化工学院,天津 300072;2. 天津医科大学总医院,天津,300052;3. 天津药物研究院,天津,300193;4. 天津市医药科学研究所,天津,300020 |
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| 摘 要： | 目的设计合成吡咯并嘧啶类化合物并研究其抑制JAK3激酶的活性。方法以4-氯-7H-吡咯并[2,3-d]嘧啶为原料,经过取代、氨基脱保护和N-酰化反应合成两类(Ⅰa和Ⅰb)吡咯并嘧啶类化合物,经体外细胞试验测定其对JAK3激酶的抑制活性。结果设计并合成了8个新化合物,结构经1H-NMR和HR-MS确证。初步活性测试结果显示Ⅰa-1和Ⅰb-3对JAK3的抑制强度与阳性对照药tofacitinib相近。结论目标化合物对JAK3依赖的DAUDI细胞抑制活性较好,对非JAK3依赖的BT-20细胞抑制作用弱。
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| 关 键 词： | JAK3激酶抑制剂 吡咯并嘧啶 合成 |
| 收稿时间： | 2016-12-20 |
Synthesis of pyrrolopyrimidines and their JAK3 inhibitory activities |
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| ZHI Shuang,YANG Miao,SHANG Qian,TAO Zun-wei and LIU Deng-ke. Synthesis of pyrrolopyrimidines and their JAK3 inhibitory activities[J]. Drugs & Clinic, 2017, 32(4): 557-561. DOI: 10.7501/j.issn.1674-5515.2017.04.002 |
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| Authors: | ZHI Shuang YANG Miao SHANG Qian TAO Zun-wei LIU Deng-ke |
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| Affiliation: | Tianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, China;School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;General Hospital Affiliated to Tianjin Medical University, Tianjin 300052, China;Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;Tianjin Institute of Medical and Pharmaceutical Sciences, Tianjin 300020, China;Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China |
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| Abstract: | Objective To design and synthesize pyrrolopyrimidines and study their JAK3 inhibitory activities. Methods The two kinds of pyrrolopyrimidines (Ia and Ib)were synthesized from 4-chloro-7H-pyrrolo[2,3-d]pyrimidine via substitution reaction, amino deprotection, and N-acetylation reaction. Their JAK3 inhibitory activities were tested by in vitro cell assay. Results Eight novel compounds were synthesized and their structures were confirmed by 1H-NMR and HR-MS. The in vitro activity experiments showed that compounds Ia-1 and Ib-3 had good inhibition against JAK3, and it was near to control drug tofacitinib. Conclusion Target compounds had good inhibition on JAK3-depended DAUDI cells, and rarely inhibition on non-JAK3-depended BT-20 cells. |
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| Keywords: | JAK3 inhibitor pyrrolopyrimidine synthesis |
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