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

Abstract A novel class of acetylhydrazone derivatives ( 5a–x ) containing 2-(phenylthiomethyl)-1 H -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)-1 H -benzo[ d ]-imidazol-1-yl)acetohydrazide ( 5a ) and N -(5-bromo-2-hydroxy-benzylidene)-2-(2-(phenylthiomethyl)-1 H -benzo[ d ]-imidazol-1-yl)acetohydrazide ( 5d ) which displayed excellent cancer inhibitory activity against the tested cancer cells (IC 50 4–17 μM), compared with 5-FU and SU11248. The others have moderate to weak inhibitory activity against the tested cancer cell lines.