Bioorganic & medicinal chemistry letters

Amide-based derivatives of β-alanine hydroxamic acid as histone deacetylase inhibitors: Attenuation of potency through resonance effects

V Liao, T Liu, R Codd

文献索引：Liao, Vivian; Liu, Tao; Codd, Rachel Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 19 p. 6200 - 6204

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被引用次数: 6

摘要

A library of amide-linked derivatives of β-alanine hydroxamic acid were prepared (2–7) and the activity as inhibitors of Zn (II)-containing histone deacetylases (HDACs) determined in vitro against HDAC1 and the anti-proliferative activity determined in BE (2)-C neuroblastoma cells. The IC50 values of the best-performing compounds (3–7) against HDAC1 ranged between 38 and 84μM. The least potent compound (2) inhibited a maximum of only 40% ...