Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors
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- 作者：Rita Scarpelli ; Annalise Di Marco ; Federica Ferrigno ; Ralph Laufer ; Isabella Marcucci ; Ester Muraglia ; Jesus M. Ontoria ; Michael Rowley ; Sergio Serafini ; Christian Steinkü ; hler ; Philip Jones
- 关键词：Histone deacetylase ; HDAC ; Trifluoroacetyl ketones
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：1 December 2008
- 年：2008
- 卷：18
- 期：23
- 页码：6078-6082
- 全文大小：189 K
文摘
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.