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

A series of imidazole and benzimidazole compounds were designed, synthesized, and found to be nanomolar inhibitors of human histone deacetylases, displaying activity in cellular and xenograft models. A series of N-hydroxy-3-[3-(1-substituted-1 H-benzoimidazol-2-yl)-phenyl]-acrylamides ( 5a– 5ab) and...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (10), p.3138-3141
Hauptverfasser:	Bressi, Jerome C., Jong, Ron de, Wu, Yiqin, Jennings, Andy J., Brown, Jason W., O’Connell, Shawn, Tari, Leslie W., Skene, Robert J., Vu, Phong, Navre, Marc, Cao, Xiaodong, Gangloff, Anthony R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylation Animals Antineoplastic agents Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Cell Line, Tumor General aspects HDAC Histone deacetylase inhibitors Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - chemistry Histone Deacetylase Inhibitors - pharmacology Histone Deacetylases - chemistry Histone Deacetylases - metabolism HL-60 Cells Humans Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Medical sciences Mice Mice, Nude Oncology Pharmacology. Drug treatments Structure-Activity Relationship Xenograft Model Antitumor Assays
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