Carbonyl-and sulfur-containing analogs of suberoylanilide hydroxamic acid: Potent inhibition of histone deacetylases

W Gu, I Nusinzon, RD Smith, CM Horvath…

Index: Gu, Wenxin; Nusinzon, Inna; Smith Jr., Ronald D.; Horvath, Curt M.; Silverman, Richard B. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 10 p. 3320 - 3329

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Citation Number: 38

Abstract

Suberoylanilide hydroxamic acid (SAHA), an inhibitor of histone deacetylase, is used in clinical trials for a variety of advanced cancers. Twelve new analogs of SAHA were synthesized and tested as in vitro inhibitors of isolated histone deacetylases (HDACS) and in vivo inhibitors of interferon regulated transcriptional responses (a marker for HDAC activity). The analogs containing an α-mercaptoketone or an α-thioacetoxyketone were ...