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Novel curcumin analogue hybrids: Synthesis and anticancer activity

TitleNovel curcumin analogue hybrids: Synthesis and anticancer activity
Publication TypeJournal Article
Year of Publication2018
AuthorsWang, JQ, Wang, X, Wang, Y, Tang, WJ, Shi, JB, Liu, XH
JournalEur J Med Chem
Date PublishedAug 5
ISBN Number0223-5234
Accession Number30025345
KeywordsAnticancer activity, Antineoplastic Agents/chemical synthesis/*chemistry/*pharmacology, Apoptosis/drug effects, Cell Cycle/drug effects, Cell Line, Tumor, Cell Proliferation/drug effects, Curcumin hybrids, Curcumin/*analogs & derivatives/chemical synthesis/*pharmacology, Humans, Membrane Potential, Mitochondrial/drug effects, Mitochondria/drug effects/metabolism, Neoplasms/*drug therapy/metabolism, Reactive Oxygen Species/metabolism, Signal Transduction/drug effects, Stomach Neoplasms/drug therapy/metabolism, Synthesis, Thioredoxin Reductase 1/antagonists & inhibitors/metabolism, 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.