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

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Liu T, Sun C, Xing X, Jing L, Tan R, Luo Y, Huang W, Song H, Li Z, Zhao Y

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

Bioorg Med Chem Lett. 2012 May 1;22(9):3122-5. doi: 10.1016/j.bmcl.2012.03.061. Epub 2012 Mar 21.

PubMed ID

22483608 [ View in PubMed

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Abstract

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)ac etohydrazide (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 (IC(50) 4-17 muM), compared with 5-FU and SU11248. The others have moderate to weak inhibitory activity against the tested cancer cell lines.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Etoposide	DNA topoisomerase 2-alpha	IC 50 (nM)	21800	N/A	N/A	Details