2. Academic Validation
  3. Benzofused hydroxamic acids: useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-fluorobenzothiophenes and benzofurans

Benzofused hydroxamic acids: useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-fluorobenzothiophenes and benzofurans

  • Bioorg Med Chem Lett. 2015 Apr 1;25(7):1603-6. doi: 10.1016/j.bmcl.2015.02.007.
Elena Marastoni 1,  Sandra Bartoli 1,  Marco Berettoni 1,  Amalia Cipollone 1,  Alessandro Ettorre 1,  Christopher I Fincham 1,  Sandro Mauro 1,  Marielle Paris 1,  Marina Porcelloni 1,  Mario Bigioni 1,  Monica Binaschi 1,  Federica Nardelli 1,  Massimo Parlani 1,  Carlo A Maggi 2,  Paola Paoli 3,  Patrizia Rossi 3,  Daniela Fattori 4
Affiliations

Affiliations

  • 1 Menarini Ricerche, Via Tito Speri 10, 00040 Pomezia (Rome), Italy.
  • 2 Menarini Ricerche, Via Rismondo12A, 50131 Florence, Italy.
  • 3 Dip. di Ingegneria Industriale, Università degli Studi di Firenze, Via Santa Marta 3, 50139 Florence, Italy.
  • 4 Menarini Ricerche, Via Tito Speri 10, 00040 Pomezia (Rome), Italy. Electronic address: dfattori@menarini-ricerche.it.
PMID: 25746815 DOI: 10.1016/j.bmcl.2015.02.007
Abstract

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.

Keywords

Fragment approach; HDAC; Hydroxamic acids.

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