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

…, AJ Jennings, JW Brown, S O'Connell, LW Tari…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 10 p. 3138 - 3141

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被引用次数: 23

摘要

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 EC50s of 20– 100nM in human A549, HL60, and PC3 cells, in vitro and in vivo hyperacetylation of ...