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Design,synthesis and biological evaluation of some novel <Emphasis Type="Italic">N</Emphasis>-arylpyrazole derivatives bearing the sulfonamide moiety as cytotoxic agents
Authors:Xiaobo Duan  Yingxing Wang  Weipei Feng  Yaxing Yang  Hongyan Li  Shenghui Li  Xiaobing Yang  Jinchao Zhang  Shuxiang Wang  Guoqiang Zhou  Chuanqi Zhou
Institution:1.Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science,Hebei University,Baoding,China;2.Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education,Hebei University,Baoding,China
Abstract: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.
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