期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 23, 页码 6083-6087出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.09.076
关键词
HDAC; Inhibitors; Trifluoroacetyl; Oxadiazoles
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. (C) 2008 Elsevier Ltd. All rights reserved.
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