1. Synthesis and Anticancer Evaluation of 4-Anilinoquinolinylchalcone Derivatives.
- Author
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Yang CY, Lee MY, Chen YL, Shiau JP, Tsai YH, Yang CN, Chang HW, and Tseng CH
- Subjects
- Humans, Female, Cell Line, Tumor, Cell Proliferation, Drug Screening Assays, Antitumor, Reactive Oxygen Species pharmacology, Apoptosis, Structure-Activity Relationship, Molecular Structure, Breast Neoplasms metabolism, Antineoplastic Agents therapeutic use
- Abstract
A series of 4-anilinoquinolinylchalcone derivatives were synthesized and evaluated for antiproliferative activities against the growth of human cancer cell lines (Huh-7 and MDA-MB-231) and normal lung cells (MRC-5). The results exhibited low cytotoxicity against human lung cells (MRC-5). Among them, ( E )-3-{4-{[4-(benzyloxy)phenyl]amino}quinolin-2-yl}-1-(4-methoxyphenyl) prop-2-en-1-one ( 4a ) was found to have the highest cytotoxicity in breast cancer cells and low cytotoxicity in normal cells. Compound 4a causes ATP depletion and apoptosis of breast cancer MDA-MB-231 cells and triggers reactive oxygen species (ROS)-dependent caspase 3/7 activation. In conclusion, it is worth studying 4-anilinoquinolinylchalcone derivatives further as new potential anticancer agents for the treatment of human cancers.
- Published
- 2023
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