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Novel Aminophenyl Benzamide-Type Histone Deacetylase Inhibitors with Enhanced Potency and Selectivity

2007; American Chemical Society; Volume: 50; Issue: 23 Linguagem: Inglês

10.1021/jm701079h

1520-4804

Oscar Moradei, Tammy C. Mallais, Sylvie Fréchette, Isabelle Paquin, Pierre Tessier, Silvana Leit, Marielle Fournel, Claire Bonfils, Marie-Claude Trachy-Bourget, Jianhong Liu, Theresa P. Yan, Aihua Lu, Jubrail Rahil, Jinru Wang, Sylvain Lefèbvre, Zuomei Li, Arkadii Vaisburg, Jeffrey M. Besterman,

Peptidase Inhibition and Analysis

Significant effort is being made to understand the role of HDAC isotypes in human cancer and to develop antitumor agents with better therapeutic windows. A part of this endeavor was the exploration of the 14 A internal cavity adjacent to the enzyme catalytic site, which led to the design and synthesis of compound 4 with the unusual bis(aryl)-type pharmacophore. SAR studies around this lead resulted in optimization to potent, selective, nonhydroxamic acid HDAC inhibitors.