Synthesis and Anticancer Evaluation of 4-Anilinoquinolinylchalcone Derivatives

Author:

Yang Cheng-Yao1,Lee Min-Yu2,Chen Yeh-Long1,Shiau Jun-Ping3,Tsai Yung-Hsiang4ORCID,Yang Chia-Ning5,Chang Hsueh-Wei67ORCID,Tseng Chih-Hua89101112ORCID

Affiliation:

1. Department of Medicinal and Applied Chemistry, College of Life Science, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan

2. Graduate Institute of Medicine, College of Medicine, Kaohsiung Medical University, Kaohsiung 80708, Taiwan

3. Division of Breast Oncology and Surgery, Department of Surgery, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, Taiwan

4. Department of Seafood Science, National Kaohsiung University of Science and Technology, Kaohsiung 811213, Taiwan

5. Institute of Precision Medicine, National Sun Yat-sen University, Kaohsiung 80424, Taiwan

6. Department of Biomedical Science and Environmental Biology, College of Life Science, Kaohsiung Medical University, Kaohsiung 80708, Taiwan

7. Center for Cancer Research, Kaohsiung Medical University, Kaohsiung 80708, Taiwan

8. Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan

9. School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan

10. Department of Medical Research, Kaohsiung Medical University Hospital, Kaohsiung City 80708, Taiwan

11. Department of Pharmacy, Kaohsiung Municipal Ta-Tung Hospital, Kaohsiung City 80145, Taiwan

12. College of Professional Studies, National Pingtung University of Science and Technology, Pingtung County 912301, Taiwan

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.

Funder

Ministry of Science and Technology of the Republic of China

Kaohsiung Medical University

Department of Pharmacy, Kaohsiung Municipal Ta-Tung Hospital

Publisher

MDPI AG

Subject

Inorganic Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Computer Science Applications,Spectroscopy,Molecular Biology,General Medicine,Catalysis

Cited by 2 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3