Optimization of a series of potent and selective ketone histone deacetylase inhibitors

The optimization of a series of ketone small molecule HDAC inhibitors leading to potent and selective class I HDAC inhibitors with good dog PK is reported. Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy and the first generation HDAC inhibitors are currently in th...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-10, Vol.18 (20), p.5528-5532
Hauptverfasser:	Pescatore, Giovanna, Kinzel, Olaf, Attenni, Barbara, Cecchetti, Ottavia, Fiore, Fabrizio, Fonsi, Massimiliano, Rowley, Michael, Schultz-Fademrecht, Carsten, Serafini, Sergio, Steinkühler, Christian, Jones, Philip
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Alkyl ketone Animals Antineoplastic agents Biological and medical sciences Cell Proliferation Dogs Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General aspects HDAC inhibitors HeLa Cells Histone Deacetylase 1 Histone Deacetylase Inhibitors Histone Deacetylases - metabolism Humans Inhibitory Concentration 50 Ketones - chemistry Medical sciences Models, Chemical Pharmacology. Drug treatments Rats Recombinant Proteins - chemistry Zinc - chemistry Zinc binding group
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Zusammenfassung:	The optimization of a series of ketone small molecule HDAC inhibitors leading to potent and selective class I HDAC inhibitors with good dog PK is reported. Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy and the first generation HDAC inhibitors are currently in the clinic. Herein we describe the optimization of a series of ketone small molecule HDAC inhibitors leading to potent and selective class I HDAC inhibitors with good dog PK.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.09.003