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Synthesis and biological evaluation of 3-(2,4-dichlorophenoxymethyl)-1-phenyl-1H-pyrazole derivatives as potential antitumor agents

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Series of novel 3-(2,4-dichlorophenoxymethyl)-1-phenyl-1H-pyrazole derivatives with various substituents at positions 4 and 5 were synthesized. Antitumor activity of all the synthesized compounds was evaluated by using SRB assay on four… Click to show full abstract

Series of novel 3-(2,4-dichlorophenoxymethyl)-1-phenyl-1H-pyrazole derivatives with various substituents at positions 4 and 5 were synthesized. Antitumor activity of all the synthesized compounds was evaluated by using SRB assay on four cell lines: lung carcinoma (A549), human hepatocellular carcinoma (HepG2), colon carcinoma (HCT116) and mammary gland breast cancer (MCF-7) cell lines. Some of the synthesized compounds showed promising activity in comparison with doxorubicin against lung carcinoma cell lines. Incorporating arylidene moiety at position-4 in pyrazole ring improved and displayed strong effect on the cytotoxic activity. Compound 9c incorporating 4-chlorophenyl moiety was the most potent toward all tested cell lines.

Keywords: pyrazole derivatives; cell lines; phenyl pyrazole; dichlorophenoxymethyl phenyl

Journal Title: Journal of the Iranian Chemical Society
Year Published: 2020

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