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


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


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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

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. Benzobthiophen-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





Autor: 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,*

Fuente: http://mdpi.com/



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