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Molecules 2017, 22(3), 467; doi:10.3390/molecules22030467

Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents in HepG-2 Cell Line

Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China
Department of Pharmacology, Shantou University Medical College, Shantou 515041, Guangdong, China
Department of Hepatobiliary Surgery II, Zhujiang Hospital of Southern Medical University, Guangzhou 510280, Guangdong, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Received: 28 February 2017 / Revised: 9 March 2017 / Accepted: 9 March 2017 / Published: 16 March 2017
View Full-Text   |   Download PDF [3969 KB, uploaded 16 March 2017]   |  


Cancer is a major public health concern worldwide. Adverse effects of cancer treatments still compromise patients’ quality of life. To identify new potential anticancer agents, a series of novel pyrazoline derivatives were synthesized and evaluated for cytotoxic effects on HepG-2 (human liver hepatocellular carcinoma cell line) and primary hepatocytes. Compound structures were confirmed by 1H-NMR, mass spectrometry, and infrared imaging. An in vitro assay demonstrated that several compounds exerted cytotoxicity in the micromolar range. Benzo[b]thiophen-2-yl-[5-(4-hydroxy-3,5-dimethoxy-phenyl)-3-(2-hydroxy-phenyl)-4,5-dihydo-pyrazol-1-yl]-methanone (b17) was the most effective anticancer agent against HepG-2 cells owing to its notable inhibitory effect on HepG-2 with an IC50 value of 3.57 µM when compared with cisplatin (IC50 = 8.45 µM) and low cytotoxicity against primary hepatocytes. Cell cycle analysis and apoptosis/necrosis evaluation using this compound revealed that b17 notably arrested HepG-2 cells in the G2/M phase and induced HepG-2 cells apoptosis. Our findings indicate that compound b17 may be a promising anticancer drug candidate. View Full-Text
Keywords: pyrazoline; anticancer activity; HepG-2 cells; apoptosis pyrazoline; anticancer activity; HepG-2 cells; apoptosis

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Xu, W.; Pan, Y.; Wang, H.; Li, H.; Peng, Q.; Wei, D.; Chen, C.; Zheng, J. Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents in HepG-2 Cell Line. Molecules 2017, 22, 467.

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