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