Synthesis and Biological Evaluation of Amino Chalcone Derivatives as Antiproliferative Agents
Chao-Fan Lu,
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,
Sai-Yang Zhang
Affiliations
Chao-Fan Lu
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Sheng-Hui Wang
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Xiao-Jing Pang
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Ting Zhu
School of Pharmaceutical Sciences, Institute of Drug Discovery & Development, Key Laboratory of Advanced Drug Preparation Technologies (Ministry of Education), Zhengzhou University, Zhengzhou 450001, China
Hong-Li Li
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Qing-Rong Li
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Qian-Yu Li
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Yu-Fan Gu
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Zhao-Yang Mu
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Min-Jie Jin
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Yin-Ru Li
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Yang-Yang Hu
Faculty of Science, The University of Melbourne, Melbourne VIC 3010, Australia
Yan-Bing Zhang
School of Pharmaceutical Sciences, Institute of Drug Discovery & Development, Key Laboratory of Advanced Drug Preparation Technologies (Ministry of Education), Zhengzhou University, Zhengzhou 450001, China
Jian Song
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
Sai-Yang Zhang
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
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.