Novel curcumin analogue hybrids: Synthesis and anticancer activity

European Journal of Medicinal Chemistry
Jie Quan WangXin Hua Liu

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.

Citations

May 17, 2019·Expert Opinion on Drug Discovery·Eirini Chainoglou, Dimitra Hadjipavlou-Litina
Mar 24, 2020·Journal of Enzyme Inhibition and Medicinal Chemistry·Xiao-Bao ShenXinhua Liu
Aug 2, 2019·Scientific Reports·Luigi MinafraGiusi Irma Forte
Nov 19, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Wamidh H TalibAsma Ismail Mahmod
Aug 8, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nicola MicaleAntonio Speciale
Aug 29, 2019·ACS Omega·Atamjit SinghPreet Mohinder Singh Bedi
Sep 8, 2021·Chemical Communications : Chem Comm·Krzysztof DzieszkowskiZbigniew Rafiński

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