Design, synthesis and biological evaluation of some novel N-arylpyrazole derivatives bearing the sulfonamide moiety as cytotoxic agents

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• 作者：Xiaobo Duan ; Yingxing Wang ; Weipei Feng ; Yaxing Yang…
• 关键词：N ; arylpyrazole ; Sulfonamide ; Anticancer ; Cytotoxicity ; Cancer cell lines
• 刊名：Research on Chemical Intermediates
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：43
• 期：1
• 页码：271-281
• 全文大小：
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Catalysis; Physical Chemistry; Inorganic Chemistry;
• 出版者：Springer Netherlands
• ISSN：1568-5675
• 卷排序：43

文摘

A series of novel N-arylpyrazole derivatives (4a–4l) bearing the sulfonamide moiety were synthesized by the condensation reaction of 1,3-dicarbonyl compounds with 4-hydrazinylbenzenesulfonamide. The structures of the obtained compounds were established on the basis of elemental (C, H, and N) and spectral analysis (1H NMR, 13C NMR, ESIMS, and FT-IR). These compounds were tested for their in vitro cytotoxic activity against three human tumor cell lines: MCF-7, Hela, and A549. The results showed that most of the obtained compounds exhibited promising cytotoxicity against the tested cell lines with low IC₅₀ values. The pyrazole derivative 4k, bearing two methoxy groups on the 3-position and 4-position of the phenyl ring, was the most effective one. Its inhibition of cell growth of MCF-7 cells was better than that of celecoxib and cisplatin.