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Identification of Novel, Selective, and Stable Inhibitors of Class II Histone Deacetylases. Validation Studies of the Inhibition of the Enzymatic Activity of HDAC4 by Small Molecules as a Novel Approach for Cancer Therapy

Jesus M. Ontoria,Sergio Altamura,Annalise Di Marco,Federica Ferrigno,Ralph Laufer,Ester Muraglia,Maria Cecilia Palumbi,Michael Rowley,Rita Scarpelli,Carsten Schultz‐Fademrecht,Sergio Serafini,Christian Steinkühler,Philip Jones

Chemistry

HDAC6

Acetylation

2009

5-Aryl-2-(trifluoroacetyl)thiophenes were identified as a new series of class II HDAC inhibitors (HDACi). Further development of this new series led to compounds such as 6h, a potent inhibitor of HDAC4 and HDAC6 (HDAC4 WT IC50 = 310 nM, HDAC6 IC50 = 70 nM) that displays 40-fold selectivity over HDAC1 and improved stability in HCT116 cancer cells (t1/2 = 11 h). Compounds 6h and 2 show inhibition of α-tubulin deacetylation in HCT116 cells at 1 μM concentration and antiproliferation effects only at concentrations where inhibition of histone H3 deacetylation is observed.

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“Identification of Novel, Selective, and Stable Inhibitors of Class II Histone Deacetylases. Validation Studies of the Inhibition of the Enzymatic Activity of HDAC4 by Small Molecules as a Novel Approach for Cancer Therapy” is a paper by Jesus M. Ontoria Sergio Altamura Annalise Di Marco Federica Ferrigno Ralph Laufer Ester Muraglia Maria Cecilia Palumbi Michael Rowley Rita Scarpelli Carsten Schultz‐Fademrecht Sergio Serafini Christian Steinkühler Philip Jones published in 2009. It has an Open Access status of “closed”. You can read and download a PDF Full Text of this paper here.