Article ID Journal Published Year Pages File Type
1364344 Bioorganic & Medicinal Chemistry Letters 2008 5 Pages PDF
Abstract

Trifluoroacetylthiophene carboxamides have recently been reported to be class II HDAC inhibitors, with moderate selectivity. Exploration of replacements for the carboxamide with bioisosteric pentatomic heteroaromatic like 1,3,4-oxadiazoles, 1,2,4-oxadiazoles and 1,3-thiazoles, led to the discovery that 2-trifluoroacetylthiophene 1,3,4-oxadiazole derivatives are very potent low nanomolar HDAC4 inhibitors, highly selective over class I HDACs (HDAC 1 and 3), and moderately stable in HCT116 cell culture.

Graphical abstractReplacement of the carboxamide moiety of trifluoroacetylthiophene HDAC4 inhibitors with bioisosteric pentatomic heteroaromatics led to the discovery of a novel series of potent and highly selective low nanomolar class II HDAC inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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