Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

  title={Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors},
  author={M G J Baud and Thomas Leiser and Vanessa Petrucci and Mekala Gunaratnam and Stephen Neidle and Franz-Josef Meyer-Almes and Matthew J Fuchter},
  booktitle={Beilstein journal of organic chemistry},
There has been significant interest in the bioactivity of the natural product psammaplin A, most recently as a potent and isoform selective HDAC inhibitor. Here we report our preliminary studies on thioester HDAC inhibitors derived from the active monomeric (thiol) form of psammaplin A, as a means to improve compound delivery into cells. We have discovered that such compounds exhibit both potent cytotoxicity and enzymatic inhibitory activity against recombinant HDAC1. The latter effect is… CONTINUE READING

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  • M G J Baud, P Haus, T Leiser, F.-J Meyer-Almes, M J Fuchter
  • ChemMedChem
  • 2013

J. Med. Chem

  • M G J Baud, T Leiser, +12 authors M J Fuchter
  • J. Med. Chem
  • 2012

Bioorg. Med. Chem

  • J García, G Franci, +6 authors A R De Lera
  • Bioorg. Med. Chem
  • 2011

Bioorg. Med. Chem. Lett

  • S Haider, C G Joseph, S Neidle, C A Fierke, M J Fuchter
  • Bioorg. Med. Chem. Lett
  • 2011

Mol. Cancer Ther

  • A Nebbioso, R Pereira, +10 authors L Altucci
  • Mol. Cancer Ther
  • 2011

J. Clin. Oncol

  • S J Whittaker, M.-F Demierre, +7 authors J Becker
  • J. Clin. Oncol
  • 2010

Angew. Chem., Int. Ed

  • L Yi, H Li, L Sun, L Liu, C Zhang, Z Xi
  • Angew. Chem., Int. Ed
  • 2009

Biochem. Pharmacol

  • S J Crabb, M Howell, +13 authors G Packham
  • Biochem. Pharmacol
  • 2008

J. Am. Chem. Soc

  • A Bowers, N West, J Taunton, S L Schreiber, J E Bradner, R M Williams
  • J. Am. Chem. Soc
  • 2008


  • T Kouzarides
  • Cell
  • 2007