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Bioorg Med Chem Lett. 2008 Dec 1;18(23):6078-82. doi: 10.1016/j.bmcl.2008.10.041. Epub 2008 Oct 12.

Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.

Author information

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

Abstract

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.

PMID:
18952417
DOI:
10.1016/j.bmcl.2008.10.041
[Indexed for MEDLINE]

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