Molecules 2017, 22(3), 467; https://doi.org/10.3390/molecules22030467
Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents in HepG-2 Cell Line
Weijie Xu 1,†
, Ying Pan 1,†, Hong Wang 1,†, Haiyan Li 2, Qing Peng 3, Duncan Wei 1, Cheng Chen 1 and Jinhong Zheng 1,*
, Ying Pan 1,†, Hong Wang 1,†, Haiyan Li 2, Qing Peng 3, Duncan Wei 1, Cheng Chen 1 and Jinhong Zheng 1,*
1
Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China
2
Department of Pharmacology, Shantou University Medical College, Shantou 515041, Guangdong, China
3
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
Abstract
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-TextKeywords:
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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