Synthesis and Anticancer Evaluation of 4-Anilinoquinolinylchalcone Derivatives.
- Resource Type
- Article
- Authors
- Yang, Cheng-Yao; Lee, Min-Yu; Chen, Yeh-Long; Shiau, Jun-Ping; Tsai, Yung-Hsiang; Yang, Chia-Ning; Chang, Hsueh-Wei; Tseng, Chih-Hua
- Source
- International Journal of Molecular Sciences. Apr2023, Vol. 24 Issue 7, p6034. 14p.
- Subject
- *CANCER cell growth
*REACTIVE oxygen species
*CANCER cells
*BREAST cancer
*ANTINEOPLASTIC agents
- Language
- ISSN
- 1661-6596
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. [ABSTRACT FROM AUTHOR]