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Alpha-keto amides as inhibitors of histone deacetylase
Carol K Wada1, Robin R Frey, Zhiqin Ji
1Cancer Research, Abbott Laboratories, Department R47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA. carol.wada@abbott.com
Bioorganic & Medicinal Chemistry Letters
|September 3, 2003
Abstract:
Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.