细胞毒性
细胞凋亡
细胞毒性T细胞
体外
化学
MCF-7型
流式细胞术
癌细胞
骨桥蛋白
药理学
细胞培养
癌症
癌症研究
生物
生物化学
人体乳房
医学
免疫学
内科学
遗传学
作者
Rahma M. Abd El-Aziz,Islam Zaki,Ibrahim M. El‐Deen,Marwa S. Abd-Rahman,Faten Z. Mohammed
出处
期刊:Anti-cancer Agents in Medicinal Chemistry
[Bentham Science]
日期:2020-11-23
卷期号:20 (18): 2304-2315
被引量:9
标识
DOI:10.2174/1871520620666200811122753
摘要
Background: Searching for new cytotoxic agents with apoptosis induction may represent a viable strategy for cancer treatment to overcome the increased resistance to available anticancer agents. Objective: The purpose of the current study was aimed at preparation and anticancer evaluation of two new series of 2H-quinolinone and halogenated 2H-quinolinone derivatives against two cancer cell lines. Methods: Two new series of 2H-quinolinone and halogenated 2H-quinolinone derivatives were prepared and screened for their cytotoxicity against breast MCF-7 and liver HepG-2 cancer cell lines as well as normal breast MCF-10a. Results: The tested molecules revealed good cytotoxicity and selectivity toward cancer cell lines relative to normal cells. These compounds were analyzed by DNA flow cytometry on MCF-7 cells. They were found to cause G2/M phase arrest and induced apoptosis at the pre-G1 phase. In addition, increased caspase 3/7 activity and decreased osteopontin expression verified the apoptotic activity. Conclusion: The potent compounds discovered in this study can be a hit for the discovery of new cytotoxic agents and are worthy of further investigation.
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