Novel Chalcone‐Phenazine Hybrids Induced Ferroptosis in U87‐MG Cells through Activating Ferritinophagy

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Abstract
Thirty‐seven novel chalcone‐phenazine hybrid molecules (C1∼C13 and F1∼F24) with 1,2,3‐triazole or ethyl group as linkers were designed and synthesized in this study. Some compounds exhibited selective cytotoxicity against U87‐MG cancer cell lines in vitro, in which compound C4 were found to have the best antiproliferative activity. SAR study indicated 1,2,3‐triazole group may be crucial for enhancing compounds’ cytotoxicity. C4 was verified to induce ferroptosis in U87‐MG cells by transcription, lipid peroxidation, lipid ROS assays. Furthermore, C4 was up‐regulated LC3‐II, degradated FTH1, and then increasing iron resulted in the down‐regulation of NCOA4. Together, all above evidences highlighted the potential of compound C4 that triggered ferroptosis by activating ferritinophagy against U87‐MG cells.
Funding Information
  • National Natural Science Foundation of China (81872757, 82273813)
  • Fundamental Research Funds for the Central Universities (2632018ZD01)

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