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Volume 25
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10.3390/molecules25235530
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Article

Synthesis and Biological Evaluation of Amino Chalcone Derivatives as Antiproliferative Agents

by
Chao-Fan Lu
1,†,
Sheng-Hui Wang
1,†,
Xiao-Jing Pang
1,2,†,
Ting Zhu
2,
Hong-Li Li
1,
Qing-Rong Li
1,
Qian-Yu Li
1,
Yu-Fan Gu
1,
Zhao-Yang Mu
1,
Min-Jie Jin
1,
Yin-Ru Li
1,
Yang-Yang Hu
3,
Yan-Bing Zhang
2,
Jian Song
1,2,* and
Sai-Yang Zhang
1,2,4,*
1
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
2
School of Pharmaceutical Sciences, Institute of Drug Discovery & Development, Key Laboratory of Advanced Drug Preparation Technologies (Ministry of Education), Zhengzhou University, Zhengzhou 450001, China
3
Faculty of Science, The University of Melbourne, Melbourne VIC 3010, Australia
4
Henan Institute of Advanced Technology, Zhengzhou University, Zhengzhou 450001, China
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Academic Editors: Jiang Wang, Liang-Ren Zhang, Peng Zhan, Qi-Dong You, Tian-Miao Ou and Xiao-Yun Lu
Molecules 2020, 25(23), 5530; https://doi.org/10.3390/molecules25235530
Received: 29 September 2020 / Revised: 23 November 2020 / Accepted: 24 November 2020 / Published: 25 November 2020
(This article belongs to the Special Issue Medicinal Chemistry in China)
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Abstract

Chalcone is a common scaffold found in many biologically active compounds. The chalcone scaffold was also frequently utilized to design novel anticancer agents with potent biological efficacy. Aiming to continue the research of effective chalcone derivatives to treat cancers with potent anticancer activity, fourteen amino chalcone derivatives were designed and synthesized. The antiproliferative activity of amino chalcone derivatives was studied in vitro and 5-Fu as a control group. Some of the compounds showed moderate to good activity against three human cancer cells (MGC-803, HCT-116 and MCF-7 cells) and compound 13e displayed the best antiproliferative activity against MGC-803 cells, HCT-116 cells and MCF-7 cells with IC50 values of 1.52 μM (MGC-803), 1.83 μM (HCT-116) and 2.54 μM (MCF-7), respectively which was more potent than the positive control (5-Fu). Further mechanism studies were explored. The results of cell colony formatting assay suggested compound 10e inhibited the colony formation of MGC-803 cells. DAPI fluorescent staining and flow cytometry assay showed compound 13e induced MGC-803 cells apoptosis. Western blotting experiment indicated compound 13e induced cell apoptosis via the extrinsic/intrinsic apoptosis pathway in MGC-803 cells. Therefore, compound 13e might be a valuable lead compound as antiproliferative agents and amino chalcone derivatives worth further effort to improve amino chalcone derivatives’ potency. View Full-Text
Keywords: chalcone; synthesis; antiproliferative; cell apoptosis chalcone; synthesis; antiproliferative; cell apoptosis
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MDPI and ACS Style

Lu, C.-F.; Wang, S.-H.; Pang, X.-J.; Zhu, T.; Li, H.-L.; Li, Q.-R.; Li, Q.-Y.; Gu, Y.-F.; Mu, Z.-Y.; Jin, M.-J.; Li, Y.-R.; Hu, Y.-Y.; Zhang, Y.-B.; Song, J.; Zhang, S.-Y. Synthesis and Biological Evaluation of Amino Chalcone Derivatives as Antiproliferative Agents. Molecules 2020, 25, 5530. https://doi.org/10.3390/molecules25235530

AMA Style

Lu C-F, Wang S-H, Pang X-J, Zhu T, Li H-L, Li Q-R, Li Q-Y, Gu Y-F, Mu Z-Y, Jin M-J, Li Y-R, Hu Y-Y, Zhang Y-B, Song J, Zhang S-Y. Synthesis and Biological Evaluation of Amino Chalcone Derivatives as Antiproliferative Agents. Molecules. 2020; 25(23):5530. https://doi.org/10.3390/molecules25235530

Chicago/Turabian Style

Lu, Chao-Fan, Sheng-Hui Wang, Xiao-Jing Pang, Ting Zhu, Hong-Li Li, Qing-Rong Li, Qian-Yu Li, Yu-Fan Gu, Zhao-Yang Mu, Min-Jie Jin, Yin-Ru Li, Yang-Yang Hu, Yan-Bing Zhang, Jian Song, and Sai-Yang Zhang. 2020. "Synthesis and Biological Evaluation of Amino Chalcone Derivatives as Antiproliferative Agents" Molecules 25, no. 23: 5530. https://doi.org/10.3390/molecules25235530

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