ArticleToxicology and applied pharmacology2016
A new brominated chalcone derivative suppresses the growth of gastric cancer cells in vitro and in vivo involving ROS mediated up-regulation of DR5 and 4 expression and apoptosis.
Article in Toxicology and applied pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 35 citations in OpenAlex.
- 3D-QSAR study for the development of chalcone-based inhibitors targeting ovarian cancer cells with experimental validation.Frontiers in pharmacology · 2026Article
- Marine natural product Methyl mycophenolate inhibits gastric cancer growth through regulating p53 and the downstream pathways.Cancer cell international · 2025Article
- Therapeutic potential of flavonoids in gastrointestinal cancer: Focus on signaling pathways and improvement strategies (Review).Molecular medicine reports · 2025Review
- Chalcones and Gastrointestinal Cancers: Experimental Evidence.International journal of molecular sciences · 2023Review
- Chalcone Derivatives: Role in Anticancer Therapy.Biomolecules · 2021Review
- Morusin Suppresses Cancer Cell Invasion and MMP-2 Expression through ERK Signaling in Human Nasopharyngeal Carcinoma.Molecules (Basel, Switzerland) · 2020Article
- SP600125 enhances C-2-induced cell death by the switch from autophagy to apoptosis in bladder cancer cells.Journal of experimental & clinical cancer research : CR · 2019Article
- A novel chalcone derivative S17 induces apoptosis through ROS dependent DR5 up-regulation in gastric cancer cells.Scientific reports · 2017Article
- Morusin inhibits cell proliferation and tumor growth by down-regulating c-Myc in human gastric cancer.Oncotarget · 2017Article
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Authors and funding
10 authors at 4 institutions in 3 countries.
Funding
Abstract
A new series of 20 brominated chalcone derivatives were designed, synthesized, and investigated for their effects against the growth of four cancer cell lines (EC109, SKNSH, HepG2, MGC803). Among them, compound 19 which given chemical name of H72, was the most potent one on gastric cancer cell lines (i.e. MGC803, HGC27, SGC7901) with IC50s ranged from 3.57 to 5.61μM. H72 exhibited less cytotoxicity to non-malignant gastric epithelial cells GES-1. H72 treatment of MGC803 and HGC27 induced generation of reactive oxygen species (ROS) leading to activation of caspase 9/3 cascade and mitochondria mediated apoptosis. H72 also up-regulated the expression of DR5, DR4 and BimEL, and down-regulated the expression of Bid, Bcl-xL, and XIAP. N-acetyl cysteine (NAC), a ROS scavenger completely blocked these effects of H72 in MGC803 cells. Intraperitoneal administration of H72 significantly inhibited the growth of MGC803 cells in vivo in a xenograft mouse model without observed toxicity. These results indicated that H72 is a lead brominated chalcone derivate and deserves further investigation for prevention and treatment of gastric cancer.
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