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J Med Chem. 2007 Nov 15;50(23):5543-6. Epub 2007 Oct 17.

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

Author information

1
MethylGene Inc, 7220 Frederick-Banting, Montréal, QC H4S 2A1, Canada. moradeio@methylgene.com

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.

PMID:
17941625
DOI:
10.1021/jm701079h
[Indexed for MEDLINE]

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