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 …

…, R Scarpelli, C Schultz-Fademrecht…

文献索引：Jones, Philip; Bottomley, Matthew J.; Carfi, Andrea; Cecchetti, Ottavia; Ferrigno, Federica; Lo Surdo, Paola; Ontoria, Jesus M.; Rowley, Michael; Scarpelli, Rita; Schultz-Fademrecht, Carsten; Steinkuehler, Christian Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 11 p. 3456 - 3461

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被引用次数: 35

摘要

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 (t 1/2= 11 h). Compounds 6h and 2 show inhibition of α-tubulin deacetylation in HCT116 ...