Benzofused hydroxamic acids: useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-fluorobenzothiophenes and benzofurans
| Autor: | Sandra Bartoli, Amalia Cipollone, Mario Bigioni, Marco Berettoni, Alessandro Ettorre, Carlo Alberto Maggi, Christopher I. Fincham, Federica Nardelli, Marina Porcelloni, Daniela Fattori, Paola Paoli, Patrizia Rossi, Monica Binaschi, Sandro Mauro, Marielle Paris, Elena Marastoni, Massimo Parlani |
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| Rok vydání: | 2014 |
| Předmět: |
Models
Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Thiophenes Hydroxamic Acids Biochemistry Histone Deacetylases chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Humans Molecular Biology Benzofurans Dose-Response Relationship Drug Molecular Structure Organic Chemistry Benzothiophene Ligand (biochemistry) Selective cytotoxicity HCT116 Cells In vitro Histone Deacetylase Inhibitors chemistry Molecular Medicine Histone deacetylase |
| Zdroj: | Bioorganicmedicinal chemistry letters. 25(7) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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