Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity

…, M Fournel, C Bonfils, MC Trachy-Bourget…

Index: Moradei, Oscar M.; Mallais, Tammy C.; Frechette, Sylvie; Paquin, Isabelle; Tessier, Pierre E.; Leit, Silvana M.; Fournel, Marielle; Bonfils, Claire; Trachy-Bourget, Marie-Claude; Liu, Jianhong; Yan, Theresa P.; Lu, Ai-Hua; Rahil, Jubrail; Wang, James; Lefebvre, Sylvain; Li, Zuomei; Vaisburg, Arkadii F.; Besterman, Jeffrey M. Journal of Medicinal Chemistry, 2007 , vol. 50, # 23 p. 5543 - 5546

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Citation Number: 105

Abstract

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 Å 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, ...