Document Report Card

ID: ALA1138236

Journal: J Med Chem

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

Authors: Moradei OM, Mallais TC, Frechette S, Paquin I, Tessier PE, Leit SM, Fournel M, Bonfils C, Trachy-Bourget MC, Liu J, Yan TP, Lu AH, Rahil J, Wang J, Lefebvre S, Li Z, Vaisburg AF, Besterman JM.

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 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.

CiteXplore: 17941625

DOI: 10.1021/jm701079h