Benzo[b]thiophene-based histone deacetylase inhibitors

David J. Witter, Sandro Belvedere, Liqiang Chen, J. Paul Secrist, Ralph T. Mosley, Thomas A. Miller

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

Abstract

Benzo[b]thienyl hydroxamic acids, a novel class of histone deacetylase (HDAC) inhibitors, were identified via a targeted screen of small molecule hydroxamic acids. Various substitutions were explored in the C5- and C6-positions of the benzo[b]thiophene core to characterize SAR and develop optimal inhibitors. It was determined that substitution at the C6-position of the benzo[b]thiophene core with a three-atom spacer yielded optimal HDAC1 inhibition and anti-proliferative activity in murine erythroleukemia (SC-9) cells.

Original languageEnglish (US)
Pages (from-to)4562-4567
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number16
DOIs
StatePublished - Aug 15 2007

Bibliographical note

Copyright:
Copyright 2009 Elsevier B.V., All rights reserved.

Keywords

  • Anticancer drug
  • Benzo[b]thiophene
  • HDAC
  • HDAC inhibitor
  • Histone deacetylase inhibitor
  • Hydroxamic acids
  • SAHA

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