Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors

We have identified a series of diphenylmethylene hydroxamic acids as novel and selective HDAC class IIa inhibitors. N-Hydroxy-2,2-diphenylacetamide ( 6), has class IIa HDAC inhibitory activity in the sub-micromolar range, while the rigidified N-hydroxy-9 H-xanthene-9-carboxamide ( 13), is slightly m...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-10, Vol.19 (19), p.5684-5688
Hauptverfasser:	Tessier, Pierre, Smil, David V., Wahhab, Amal, Leit, Silvana, Rahil, Jubrail, Li, Zuomei, Déziel, Robert, Besterman, Jeffrey M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Analytical, structural and metabolic biochemistry Biological and medical sciences Cell Line Diphenylacetic Acids - chemical synthesis Diphenylacetic Acids - chemistry Diphenylacetic Acids - pharmacology Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology HDAC class IIa selective inhibitors HDAC inhibitors HDAC4 inhibitors HDAC5 inhibitors HDAC7 inhibitors Histone Deacetylases - metabolism Humans Hydrolases Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology Medical sciences Miscellaneous Pharmacology. Drug treatments Protein Isoforms - antagonists & inhibitors Protein Isoforms - metabolism Structure-Activity Relationship Xanthenes - chemical synthesis Xanthenes - chemistry Xanthenes - pharmacology
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