2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 11, 2008, Pages 3456-3461

  Jones, Philip ^a   Bottomley, Matthew J ^a   Carfí, Andrea ^a   Cecchetti, Ottavia ^a   Ferrigno, Federica ^a   Lo Surdo, Paola ^a   Ontoria, Jesus M ^a   Rowley, Michael ^a   Scarpelli, Rita ^a   Schultz Fademrecht, Carsten ^a   Steinkühler, Christian ^a  

^a IRBM   (Italy)

Author keywords

HDAC; Histone deacetylase; Hydrated ketones; Trifluoroacetyl ketones

Indexed keywords

2 TRIFLUOROACETYLTHIOPHENE DERIVATIVE; 5 (TRIFLUOROACETYL)THIOPHENE 2 CARBOXAMIDE DERIVATIVE; HISTONE DEACETYLASE 2; HISTONE DEACETYLASE 2 INHIBITOR; HISTONE DEACETYLASE INHIBITOR; THIOPHENE DERIVATIVE;

ARTICLE; CELL; DRUG ACTIVITY; DRUG BINDING; DRUG INHIBITION; DRUG POTENCY; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; HISTONE DEACETYLASES; MOLECULAR CONFORMATION; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES; ZINC;

EID: 42049121320     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.02.026     Document Type: Article

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10. 2, 0.1 mg/ml BSA), Fluor-de-Lys substrate solution was added and left for 1 h at 37 °C and the reaction stopped by adding developer/TSA solution. Measure the fluorescence at ex. 360 nM/em. 460 nM.
11. 2, 0.1 mg/ml BSA), trifluoacetamide substrate solution was added and left for 1 h at 37 °C and the reaction stopped by adding developer/TSA solution. Measure the fluorescence at ex. 360 nM/em. 460 nM.
12. Compound 1 was purchased from Rieke Metals, Lincoln, USA.
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