Author/Authors :
Charles M. Marson، نويسنده , , Thevaki Mahadevan، نويسنده , , Jon Dines، نويسنده , , Stéphane Sengmany، نويسنده , , James M. Morrell، نويسنده , , John P. Alao، نويسنده , , Simon P. Joel، نويسنده , , David M. Vigushin، نويسنده , , R. Charles Coombes، نويسنده ,
Abstract :
Syntheses of aryloxyalkanoic acid hydroxyamides are described, all of which are potent inhibitors of histone deacetylase, some being more potent in vitro than trichostatin A (IC50 = 3 nM). Variation of the substituents on the benzene ring as well as fusion of a second ring have marked effects on potency, in vitro IC50 values down to 1 nM being obtained.
Keywords :
Histone deacetylase , Enzyme inhibitors , hydroxamic acids , Aryloxyalkanoic acid derivatives
