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. 2006 May 15;14(10):3320-9.
doi: 10.1016/j.bmc.2005.12.047. Epub 2006 Jan 24.

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

Wenxin Gu  1 , Inna Nusinzon, Ronald D Smith Jr, Curt M Horvath, Richard B Silverman
Affiliations

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

Wenxin Gu et al. Bioorg Med Chem. .

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 alpha-mercaptoketone or an alpha-thioacetoxyketone were more potent than SAHA in both assays.

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