Synthesis and Anticancer Evaluation of 4-Anilinoquinolinylchalcone Derivatives

Autor:	Cheng-Yao Yang, Min-Yu Lee, Yeh-Long Chen, Jun-Ping Shiau, Yung-Hsiang Tsai, Chia-Ning Yang, Hsueh-Wei Chang, Chih-Hua Tseng
Jazyk:	angličtina
Rok vydání:	2023
Předmět:	4-anilinoquinolinylchalcone lapatinib cytotoxicity reactive oxygen species apoptosis Biology (General) QH301-705.5 Chemistry QD1-999
Zdroj:	International Journal of Molecular Sciences, Vol 24, Iss 7, p 6034 (2023)
Druh dokumentu:	article
ISSN:	1422-0067 1661-6596
DOI:	10.3390/ijms24076034
Popis:	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.
Databáze:	Directory of Open Access Journals
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