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.
Highlights
Worldwide, liver cancer is the third most common cause of cancer deaths
We describe the synthesis of new pyrazoline derivatives (b1–19)
We found that compound b17 was the most effective anticancer agent following a 48 h exposure with an IC50 value of 3.57 μM compared with the cisplatin value of 8.45 μM
Summary
Liver cancer is the third most common cause of cancer deaths. It is the fifth and seventh most common cancer in men and women, respectively [1]. (II) is a selective p38α mitogen-activated protein kinase (MAPK) inhibitor undergoing Phase III clinical trials Axitinib [13,14]. (III), a vascular growth factor receptor inhibitor, used in clinical treatment, is exploited by Pfizer [15,16]. (IV), inhibitor, a VEGFR used in clinical treatment, is exploited by Pfizer [15,16]. Pazopanib (IV), a VEGFR inhibitor, is exploited by GlaxoSmithKline [17,18]. 0 -hydroxymethyl-2’-furyl)-1-benzyl indazole (YC-1) (VI) is a hypoxia-inducible inhibitor [19,20]. [19,20] and 3-(5′-hydroxymethyl-2’-furyl)-1-benzyl indazole (YC-1) (VI) is a hypoxia-inducible factor factor inhibitor as awell as inhibitor a VEGF [21,22]. We describe the synthesis of new pyrazoline derivatives (b1–19).
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