2. Academic Validation
  3. Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity

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

  • J Med Chem. 2007 Nov 15;50(23):5543-6. doi: 10.1021/jm701079h.
Oscar M Moradei 1,  Tammy C Mallais,  Sylvie Frechette,  Isabelle Paquin,  Pierre E Tessier,  Silvana M Leit,  Marielle Fournel,  Claire Bonfils,  Marie-Claude Trachy-Bourget,  Jianhong Liu,  Theresa P Yan,  Ai-Hua Lu,  Jubrail Rahil,  James Wang,  Sylvain Lefebvre,  Zuomei Li,  Arkadii F Vaisburg,  Jeffrey M Besterman
Affiliations

Affiliation

  • 1 MethylGene Inc, 7220 Frederick-Banting, Montréal, QC H4S 2A1, Canada. [email protected]
PMID: 17941625 DOI: 10.1021/jm701079h
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.

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