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Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group

Academic Article
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Overview

related to degree

  • Wu, Tom, Ph.D. in Chemistry, Scripps Research 2000 - 2003

authors

  • Wu, Tom
  • Hassig, Christian
  • Wu, Y. Q.
  • Ding, Sheng
  • Schultz, Peter

publication date

  • January 2004

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • Histone deacetylases (HDAC) are promising targets for cancer chemotherapy. HDAC inhibitors are thought to act in part by disrupting normal cell cycle regulation, resulting in apoptosis and/or differentiation of transformed cells. Several HDAC inhibitors, which contain hydrophobic tails and the Zn(2+) chelator hydroxyamic acid as a head group, are potent inhibitors of HDACs both in vitro and in vivo. In this study, a related class of compounds with a N-formyl hydroxylamino head group has been synthesized and their ability to inhibit HDACs have been assayed in biochemical and cellular assays. These compounds were found to have comparable activities to suberoylanilide hydroxyamic acid (SAHA) in HDAC enzymatic assays and histone hyperacetylation cellular assays.

subject areas

  • Drug Design
  • Enzyme Inhibitors
  • HeLa Cells
  • Histone Deacetylase Inhibitors
  • Histone Deacetylases
  • Humans
  • Hydroxylamine
  • Jurkat Cells
  • U937 Cells
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2003.10.055

PubMed ID

  • 14698179
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Additional Document Info

start page

  • 449

end page

  • 453

volume

  • 14

issue

  • 2

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