Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors

A number of potent (IC 50 = 10–200 nM) and highly selective HDAC6 inhibitors are reported. In an effort to identify HDAC isoform selective inhibitors, we designed and synthesized novel, chiral 3,4-dihydroquinoxalin-2(1 H)-one and piperazine-2,5-dione aryl hydroxamates showing selectivity (up to 40-f...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-02, Vol.19 (3), p.688-692
Hauptverfasser:	Smil, David V., Manku, Sukhdev, Chantigny, Yves A., Leit, Silvana, Wahhab, Amal, Yan, Theresa P., Fournel, Marielle, Maroun, Christiane, Li, Zuomei, Lemieux, Anne-Marie, Nicolescu, Alina, Rahil, Jubrail, Lefebvre, Sylvain, Panetta, Anthony, Besterman, Jeffrey M., Déziel, Robert
Format:	Artikel
Sprache:	eng
Schlagworte:	3,4-Dihydroquinoxalin-2(1 H)-ones Acetylation Antineoplastic agents Aryl hydroxamic acids Biological and medical sciences Catalytic Domain Chemistry, Pharmaceutical - methods Drug Design Enzyme Inhibitors - chemistry General aspects HDAC inhibitors HDAC6 Histone acetylation Histone Deacetylase 6 Histone Deacetylase Inhibitors Histone Deacetylases - chemistry Histone Deacetylases - metabolism Histones - chemistry Humans Hydroxamic Acids - pharmacology Inhibitory Concentration 50 Medical sciences Models, Chemical Pharmacology. Drug treatments Piperazine-2,5-diones Piperazines - chemistry Protein Isoforms Tubulin - chemistry Tubulin acetylation
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