新型苯基噻吩-2-基甲酮类化合物的合成及其对人脐静脉内皮细胞的保护活性

doi:10.3724/SP.J.1095.2014.30651

摘要/Abstract

摘要： 合成了13个具有新型结构的苯基(噻吩-2-基)甲酮类化合物，其中3个化合物(9b,10b,11b)未见文献报道，目标化合物的结构均经ESI-MS、1H NMR和13C NMR等技术手段进行了确证。对H2O2诱导的人脐静脉内皮细胞(HUVECs)氧化损伤保护活性的结果显示，对位甲氧基以及两个氯原子取代的活性较好。初步构效关系表明，苯基噻吩甲酮母环上取代基的位置、数目、类型是影响化合物活性的主要原因。

关键词: 苯基(噻吩-基)甲酮, 合成, 人脐静脉内皮细胞, 保护活性

Abstract: Thirteen phenyl(thiophen-2-yl)methanone derivatives were designed and synthesized by classic synthetic methods, in which compounds 9b, 10b and 11b are new. All target structures were confirmed by ESI-MS, 1H NMR and 13C NMR. Their in vitro cytoprotective activities against H2O2-induced injury on human umbilical vein endothelial cells(HUVECs) were tested. And the results show that p-methoxy groups and two chlorine atoms substituted on the phenyl ring express preferable protective activity. The preliminary structure-activity relationships results show that the position, number and type of substituents on the core structure have remarkable effects on protective activities against H2O2 induced injury on HUVECs.

Key words: phenyl(thiophen-yl)methanone, synthesis, human umbilical vein endothelial cells, cytoprotective activity

中图分类号:

O625

孔亮, 冯秀娥, 高洁, 李静, 李青山. 新型苯基噻吩-2-基甲酮类化合物的合成及其对人脐静脉内皮细胞的保护活性[J]. 应用化学, DOI: 10.3724/SP.J.1095.2014.30651.

KONG Liang, FENG Xiue*, GAO Jie, LI Jing, LI Qingshan*. Synthesis of Novel Phenyl(thiophen-2-yl)methanone Derivatives and Their Cytoprotective Activities Against H₂O₂-induced Injury in Human Umbilical Vein Endothelial Cells[J]. Chinese Journal of Applied Chemistry, DOI: 10.3724/SP.J.1095.2014.30651.

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