title: Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents in HepG-2 Cell Line.
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 IC50value 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 thatb17notably arrested HepG-2 cells in the G₂/M phase and induced HepG-2 cells apoptosis. Our findings indicate that compoundb17may be a promising anticancer drug candidate.
authors.affiliation: Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China. 13536920534@163.com.
authors.forename: Weijie
authors.initials: W
authors.lastname: Xu
authors.affiliation: Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China. ypan@stu.edu.cn.
authors.forename: Ying
authors.initials: Y
authors.lastname: Pan
authors.affiliation: Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China. 13592851552@163.com.
authors.forename: Hong
authors.initials: H
authors.lastname: Wang
authors.affiliation: Department of Pharmacology, Shantou University Medical College, Shantou 515041, Guangdong, China. 13066360950@163.com.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Li
authors.affiliation: Department of Hepatobiliary Surgery II, Zhujiang Hospital of Southern Medical University, Guangzhou 510280, Guangdong, China. zhujiangzhuanhua@163.com.
authors.forename: Qing
authors.initials: Q
authors.lastname: Peng
authors.affiliation: Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China. weiduncan2012@163.com.
authors.forename: Duncan
authors.initials: D
authors.lastname: Wei
authors.affiliation: Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China. 13411963192@163.com.
authors.forename: Cheng
authors.initials: C
authors.lastname: Chen
authors.affiliation: Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China. jhzheng@stu.edu.cn.
authors.forename: Jinhong
authors.initials: J
authors.lastname: Zheng
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000187:drug effects; D006801:Humans; D008297:Male; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011720:Pyrazoles; C031280:pyrazole
keywords: HepG-2 cells; anticancer activity; apoptosis; pyrazoline