2. Academic Validation
  3. Novel curcumin analogue hybrids: Synthesis and anticancer activity

Novel curcumin analogue hybrids: Synthesis and anticancer activity

  • Eur J Med Chem. 2018 Aug 5:156:493-509. doi: 10.1016/j.ejmech.2018.07.013.
Jie Quan Wang 1,  Xiaobin Wang 2,  Yang Wang 1,  Wen Jian Tang 1,  Jing Bo Shi 1,  Xin Hua Liu 3
Affiliations

Affiliations

  • 1 Anhui Province Key Laboratory of Major Autoimmune Diseases, Anhui Institute of Innovative Drugs, School of Pharmacy, Anhui Medical University, Hefei, 230032, PR China.
  • 2 College of Sciences, Nanjing Agricultural University, Nanjing, 210095, PR China.
  • 3 Anhui Province Key Laboratory of Major Autoimmune Diseases, Anhui Institute of Innovative Drugs, School of Pharmacy, Anhui Medical University, Hefei, 230032, PR China; School of Material Science Chemical Engineering, ChuZhou University, ChuZhou, 239000, PR China. Electronic address: xhliuhx@163.com.
PMID: 30025345 DOI: 10.1016/j.ejmech.2018.07.013
Abstract

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.

Keywords

Anticancer activity; Curcumin hybrids; Synthesis; TrxR.

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