| Literature DB >> 17941625 |
Oscar M Moradei1, 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.
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.Entities:
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Year: 2007 PMID： 17941625 DOI： 10.1021/jm701079h
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446