Chinese Journal of Applied Chemistry

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Synthesis of Novel Phenyl(thiophen-2-yl)methanone Derivatives and Their Cytoprotective Activities Against H2O2-induced Injury in Human Umbilical Vein Endothelial Cells

KONG Liang, FENG Xiue*, GAO Jie, LI Jing, LI Qingshan*   

  1. (School of Pharmaceutical Science,Shanxi Medical University,Taiyuan 030001,China)
  • Received:2013-12-23 Revised:2014-03-05 Published:2014-09-04 Online:2014-09-04

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

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