Novel curcumin analogue hybrids: Synthesis and anticancer activity

作者：Wang, Jie Quan; Wang, Xiaobin; Wang, Yang; Tang, Wen Jian; Shi, Jing Bo; Liu, Xin Hua^*

来源：European Journal of Medicinal Chemistry, 2018, 156: 493-509.

DOI：10.1016/j.ejmech.2018.07.013

• Synthesis
• Curcumin hybrids
• Anticancer activity
• TrxR

In this study, twenty curcumin analogue hybrids as potential anticancer agents through regulation protein of TrxR were designed and synthesized. Results of anticancer activity showed that 5,7-dimethoxy-3-(3-(2-((1E, 4E)-3-oxo-5-(pyridin- 2-yl)penta-1,4-dien-1- yl)phenoxy)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one (compound 7d) could induce gastric cancer cells apoptosis by arresting cell cycle, break mitochondria function and inhibit TrxR activity. Meanwhile, western blot revealed that this compound could dramatically up expression of Bax/Bcl-2 ratio and high expression of TrxR oxidation. These results preliminarily show that the important role of ROS mediated activation of ASK1/MAPK signaling pathways by this title compound.

• 出版日期2018-8-5
• 单位安徽医科大学; 滁州学院; 南京农业大学