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ID: ALA1146704
Journal: Bioorg Med Chem Lett
Title: (2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
Authors: Vaisburg A, Bernstein N, Frechette S, Allan M, Abou-Khalil E, Leit S, Moradei O, Bouchain G, Wang J, Woo SH, Fournel M, Yan PT, Trachy-Bourget MC, Kalita A, Beaulieu C, Li Z, MacLeod AR, Besterman JM, Delorme D.
Abstract: 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 IC(50) values in the low micromolar range and induce hyperacetylation of histones in whole cells. They induced expression of p21WAF1/Cip1 and caused cell-cycle arrest in human cancer cells. Compounds in this class showed efficacy in human tumor xenograft models.
CiteXplore: 14684344