82788-34-9Relevant articles and documents
Benzofused hydroxamic acids: Useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-Fluorobenzothiophenes and benzofurans
Marastoni, Elena,Bartoli, Sandra,Berettoni, Marco,Cipollone, Amalia,Ettorre, Alessandro,Fincham, Christopher I.,Mauro, Sandro,Paris, Marielle,Porcelloni, Marina,Bigioni, Mario,Binaschi, Monica,Nardelli, Federica,Parlani, Massimo,Maggi, Carlo A.,Paoli, Paola,Rossi, Patrizia,Fattori, Daniela
, p. 1603 - 1606 (2015/03/30)
In the search for a new class of histone deacetylase inhibitors, we prepared a series of very simple benzofused hydroxamic acids to find an anchoring fragment of minimal molecular weight: they showed very good ligand efficiencies. Following these findings, classical fragment growing work was performed to increase binding energy and selective cytotoxicity. In the second phase of the work, information from the SARs of the benzothiophene series and data available in literature, we explored the in vitro pharmacological properties of the 6-substituted-7-fluoro-benzothiophene hydroxamates and the 5-susbtituted-benzofuran hydroxamates.
Inhibitors of histone deacetylase
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, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Inhibitors of histone deacetylase
-
, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.