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

Wenxin Gu, Inna Nusinzon, Ronald D. Smith, Curt M. Horvath, Richard B. Silverman*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

46 Scopus citations

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 more potent than SAHA in both assays.

Original languageEnglish (US)
Pages (from-to)3320-3329
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume14
Issue number10
DOIs
StatePublished - May 15 2006

Keywords

  • Histone deacetylase
  • Inhibitors
  • SAHA
  • Suberoylanilide hydroxamic acid
  • α-Mercaptoketone
  • α-Thioacetoxyketone

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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