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Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents

  作者 Liu, T; Sun, CY; Xing, XM; Jing, LL; Tan, R; Luo, YF; Huang, WC; Song, H; Li, ZC; Zhao, YL  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-9;  页码  3122-3125  
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[摘要]A novel class of acetylhydrazone derivatives (5a-x) containing 2-(phenylthiomethyl)-1H-benzo-[d]-imidazole moieties are synthesizer, and their antitumor activities against A549, HCT116, HepG2, PC-9, and A375 were determined by the MTT assay. Among them are N-(2,4-dihydroxybenzylidene)-2-(2-(phenylthiomethyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide (5a) and N-(5-bromo-2-hydroxy-benzylidene)-2-(2-(phenylthiomethyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide (5d) which displayed excellent cancer inhibitory activity against the tested cancer cells (IC50 4-17 mu M), compared with 5-FU and SU11248. The others have moderate to weak inhibitory activity against the tested cancer cell lines. (C) 2012 Elsevier Ltd. All rights reserved.

 
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