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Bioorg Med Chem Lett. 2008 Dec 1;18(23):6083-7. doi: 10.1016/j.bmcl.2008.09.076. Epub 2008 Sep 24.

2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.

Author information

1
IRBM-Merck Research Laboratories Rome, Via Pontina km 30,600-Pomezia, 00040 Rome, Italy. ester_muraglia@merck.com

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.

PMID:
18930398
DOI:
10.1016/j.bmcl.2008.09.076
[Indexed for MEDLINE]

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