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

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 mo...

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Published in:Bioorganic & medicinal chemistry 2008-12, Vol.18 (23), p.6078-6082
Main Authors: SCARPELLI, Rita, DI MARCO, Annalise, JONES, Philip, FERRIGNO, Federica, LAUFER, Ralph, MARCUCCI, Isabella, MURAGLIA, Ester, ONTORIA, Jesus M, ROWLEY, Michael, SERAFINI, Sergio, STEINKÜHLER, Christian
Format: Article
Language:English
Subjects:
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacology
Antineoplastic agents
Aryl Hydrocarbon Hydroxylases - antagonists & inhibitors
Biological and medical sciences
Cytochrome P-450 CYP2C9
Drug Design
General aspects
HCT116 Cells
HeLa Cells
Hepatocytes - drug effects
Histone Deacetylase Inhibitors
Histone Deacetylases - classification
Humans
Medical sciences
Microsomes, Liver - drug effects
Molecular Structure
Pharmacology. Drug treatments
Structure-Activity Relationship
Thiophenes - chemical synthesis
Thiophenes - chemistry
Thiophenes - pharmacology
Tubulin - drug effects
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Summary: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.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.10.041