849235-60-5Relevant articles and documents
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity
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.
, p. 5543 - 5546 (2007)
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 ? 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.