α-Keto amides as inhibitors of histone deacetylase

…, J Guo, KB Glaser, PA Marcotte, PL Richardson…

Index: Wada, Carol K.; Frey, Robin R.; Ji, Zhiqin; Curtin, Michael L.; Garland, Robert B.; Holms, James H.; Li, Junling; Pease, Lori J.; Guo, Jun; Glaser, Keith B.; Marcotte, Patrick A.; Richardson, Paul L.; Murphy, Shannon S.; Bouska, Jennifer J.; Tapang, Paul; Magoc, Terrance J.; Albert, Daniel H.; Davidsen, Steven K.; Michaelides, Michael R. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 19 p. 3331 - 3335

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Citation Number: 69

Abstract

α-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 α-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.