Phosphorus-based SAHA analogues as histone deacetylase inhibitors.

Galina V. Kapustin, György Fejér, Jennifer L. Gronlund, Dewey G. McCafferty, Edward Seto, Felicia A. Etzkorn*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

[structure: see text] Three analogues of suberoyl anilide hydroxamic acid (SAHA) with phosphorus metal-chelating functionalities were synthesized as inhibitors of histone deacetylases (HDACs). The compounds showed weak activity for HeLa nuclear extracts (IC(50) = 0.57-6.1 mM), HDAC8 (IC(50) = 0.28-0.41 mM), and histone-deacetylase-like protein (HDLP, IC(50) = 0.33-1.9 mM), suggesting that the transition state of HDAC is not analogous to zinc proteases. Antiproliferative activity against A2780 cancer cells (IC(50) = 0.11-0.12 mM), comparable to SAHA (0.15 mM), was observed.
Original languageEnglish
Pages (from-to)3053-3056
Number of pages0
JournalOrg Lett
Volume5
Issue number17
DOIs
Publication statusPublished - 21 Aug 2003

Keywords

  • Antineoplastic Agents
  • Bacterial Proteins
  • Cell Nucleus
  • Enzyme Inhibitors
  • Female
  • HeLa Cells
  • Histone Deacetylase Inhibitors
  • Humans
  • Hydroxamic Acids
  • Inhibitory Concentration 50
  • Organophosphorus Compounds
  • Ovarian Neoplasms
  • Recombinant Proteins
  • Tumor Cells
  • Cultured
  • Vorinostat

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