Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity.

@article{Bressi2010BenzimidazoleAI,
  title={Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity.},
  author={Jerome C Bressi and Ron de Jong and Yiqin Wu and Andy J Jennings and Jason W. Brown and Shawn O'Connell and Leslie W. Tari and Robert J Skene and Phong Vu and Marc Navre and Xiaodong Cao and Anthony R. Gangloff},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 10},
  pages={3138-41}
}
A series of N-hydroxy-3-[3-(1-substituted-1H-benzoimidazol-2-yl)-phenyl]-acrylamides (5a-5ab) and N-hydroxy-3-[3-(1,4,5-trisubstituted-1H-imidazol-2-yl)-phenyl]-acrylamides (12a-s) were designed, synthesized, and found to be nanomolar inhibitors of human histone deacetylases. Multiple compounds bearing an N1-piperidine demonstrate EC(50)s of 20-100 nM in human A549, HL60, and PC3 cells, in vitro and in vivo hyperacetylation of histones H3 and H4, and induction of p21(waf). Compound 5x displays… CONTINUE READING

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