Title of article
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors
Author/Authors
Rita Scarpelli، نويسنده , , Annalise Di Marco، نويسنده , , Federica Ferrigno، نويسنده , , Ralph Laufer، نويسنده , , Isabella Marcucci، نويسنده , , Ester Muraglia، نويسنده , , Jesus M. Ontoria، نويسنده , , Michael Rowley، نويسنده , , Sergio Serafini، نويسنده , , Christian Steinkühler، نويسنده , , Philip Jones، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
6078
To page
6082
Abstract
5-(Trifluoroacetyl)thiophene-2-carboxamides were found to be potent and selective class II HDAC inhibitors. This paper describes their further development and the investigation on the cause for the lack of cell-based activity. A rapid screening assay was set up which enabled the identification of more metabolic stable compounds as potent and selective class II HDAC inhibitors.
Keywords
Trifluoroacetyl ketones , HDAC , Histone deacetylase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800173
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