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

@inproceedings{Baud2013ThioesterDO,
  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},
  year={2013}
}
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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