Vorinostat-like molecules as structural, stereochemical, and pharmacological tools.

نویسندگان

  • Stephen Hanessian
  • Luciana Auzzas
  • Andreas Larsson
  • Jianbin Zhang
  • Giuseppe Giannini
  • Grazia Gallo
  • Andrea Ciacci
  • Walter Cabri
چکیده

The inhibitory activity of an ω-alkoxy analogue of the HDAC inhibitor, Vorinostat (SAHA), against the 11 isoforms of HDAC is described and evaluated with regard to structural biology information retrieved through computational methods. Preliminary absorption and metabolism studies were performed, which positioned this compound as a potential candidate for further preclinical studies and delineated measures for improving its pharmacokinetic profile.

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عنوان ژورنال:
  • ACS medicinal chemistry letters

دوره 1 2  شماره 

صفحات  -

تاریخ انتشار 2010