1132769-55-1Relevant articles and documents
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors
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
scheme or table, p. 688 - 692 (2009/08/15)
In an effort to identify HDAC isoform selective inhibitors, we designed and synthesized novel, chiral 3,4-dihydroquinoxalin-2(1H)-one and piperazine-2,5-dione aryl hydroxamates showing selectivity (up to 40-fold) for human HDAC6 over other class I/IIa HDACs. The observed selectivity and potency (IC50 values 10-200 nM against HDAC6) is markedly dependent on the absolute configuration of the chiral moiety, and suggests new possibilities for use of chiral compounds in selective HDAC isoform inhibition.
