New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation.

نویسندگان

  • Matthias G J Baud
  • Thomas Leiser
  • Franz-Josef Meyer-Almes
  • Matthew J Fuchter
چکیده

New synthetic routes towards the natural product psammaplin A were developed with the particular view to preparing diverse analogues for biological assessment. These routes utilize cheap and commercially available starting materials, and allowed access to psammaplin A analogues not accessible via currently reported methods. Preliminary biological studies revealed these compounds to be the most potent non peptidic inhibitors of the enzyme histone deacetylase 1 (HDAC1, class I) discovered so far. Interestingly, psammaplin A and our synthetic analogues show class I selectivity in vitro, an important feature for the design and synthesis of future isoform selective inhibitors.

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عنوان ژورنال:
  • Organic & biomolecular chemistry

دوره 9 3  شماره 

صفحات  -

تاریخ انتشار 2011