
Bioorganic and Medicinal Chemistry p. 3320 - 3329 (2006)
Update date:2022-08-04
Topics:
Gu, Wenxin
Nusinzon, Inna
Smith Jr., Ronald D.
Horvath, Curt M.
Silverman, Richard B.
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 more potent than SAHA in both assays.
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