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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2008-11-13
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:Di MarcoAnnaliseA,
pubmed-author:FerrignoFedericaF,
pubmed-author:JonesPhilipP,
pubmed-author:LauferRalphR,
pubmed-author:MarcucciIsabellaI,
pubmed-author:MuragliaEsterE,
pubmed-author:OntoriaJesus MJM,
pubmed-author:RowleyMichaelM,
pubmed-author:ScarpelliRitaR,
pubmed-author:SerafiniSergioS,
pubmed-author:SteinkühlerChristianC
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6078-82
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18952417-Amides,
pubmed-meshheading:18952417-Aryl Hydrocarbon Hydroxylases,
pubmed-meshheading:18952417-Drug Design,
pubmed-meshheading:18952417-HCT116 Cells,
pubmed-meshheading:18952417-HeLa Cells,
pubmed-meshheading:18952417-Hepatocytes,
pubmed-meshheading:18952417-Histone Deacetylase Inhibitors,
pubmed-meshheading:18952417-Histone Deacetylases,
pubmed-meshheading:18952417-Humans,
pubmed-meshheading:18952417-Microsomes, Liver,
pubmed-meshheading:18952417-Molecular Structure,
pubmed-meshheading:18952417-Structure-Activity Relationship,
pubmed-meshheading:18952417-Thiophenes,
pubmed-meshheading:18952417-Tubulin
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pubmed:year |
2008
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pubmed:articleTitle |
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
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pubmed:affiliation |
IRBM-Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia 00040, Rome, Italy. rita_scarpelli@merck.com
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pubmed:publicationType |
Journal Article
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