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(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors |
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| Authors: | Vaisburg Arkadii Bernstein Naomy Frechette Sylvie Allan Martin Abou-Khalil Elie Leit Silvana Moradei Oscar Bouchain Giliane Wang James Woo Soon Hyung Fournel Marielle Yan Pu T Trachy-Bourget Marie-Claude Kalita Ann Beaulieu Carole Li Zuomei MacLeod A Robert Besterman Jeffrey M Delorme Daniel |
| Affiliation: | Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montreal, Quebec, Canada H4S 2A1. vaisburga@methylgene.com |
| 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. |
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