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

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.
Ting Liu 1,  Changyan Sun,  Xiumei Xing,  Lingling Jing,  Rui Tan,  Youfu Luo,  Wencai Huang,  Hang Song,  Zicheng Li,  Yinglan Zhao
Affiliations

Affiliation

  • 1 Department of Pharmaceutical and Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, PR China.
PMID: 22483608 DOI: 10.1016/j.bmcl.2012.03.061
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)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 (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.

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