The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
A variety of omega-substituted alkanoic acid (2-amino-phenyl)-amides were designed and synthesized. These compounds were shown to inhibit recombinant human histone deacetylases (HDACs) with IC50 values in the low micromolar range and induce hyperacetylation of histones in whole cells. They induced expression of p21WAFl/Cip1 and caused cell-cycle arrest in human cancer cells. Compounds in this class showed efficacy in human tumor xenograft models. (C) 2003 Elsevier Ltd. All rights reserved.
INHIBITORS OF HISTONE DEACETYLASE
申请人:Methylgene, Inc.
公开号:EP1280764B1
公开(公告)日:2010-11-24
US7288567B2
申请人:——
公开号:US7288567B2
公开(公告)日:2007-10-30
Inhibitors of histone deacetylase
申请人:——
公开号:US20020115826A1
公开(公告)日:2002-08-22
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.