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Novel curcumin analogue hybrids: Synthesis and anticancer activity.

Authors :
Wang, Jie Quan
Wang, Xiaobin
Wang, Yang
Tang, Wen Jian
Shi, Jing Bo
Liu, Xin Hua
Source :
European Journal of Medicinal Chemistry. Aug2018, Vol. 156, p493-509. 17p.
Publication Year :
2018

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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
156
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
131295623
Full Text :
https://doi.org/10.1016/j.ejmech.2018.07.013