2. Academic Validation
  3. Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures

Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures

  • Bioorg Med Chem Lett. 2012 Sep 1;22(17):5360-2. doi: 10.1016/j.bmcl.2012.07.067.
Mario Bigioni 1,  Alessandro Ettorre,  Patrizia Felicetti,  Sandro Mauro,  Cristina Rossi,  Carlo Alberto Maggi,  Elena Marastoni,  Monica Binaschi,  Massimo Parlani,  Daniela Fattori
Affiliations

Affiliation

  • 1 Menarini Ricerche Pomezia, via Tito Speri 10, 00040 Pomezia, Rome, Italy.
PMID: 22877635 DOI: 10.1016/j.bmcl.2012.07.067
Abstract

We report here the strategy used in our research group to find a new class of histone deacetylase (HDAC) inhibitors. A series of 5,11-dihydrodibenzo[b,e]azepine-6-ones alkylated on the amide nitrogen with an alkyl chain bearing an hydroxamic acids moiety at the end, has been designed (based upon the general motif for HDAC inhibitors), synthesized and tested. This allowed us to identify a new series of submicromolar HDAC inhibitors, which showed antiproliferative activity on HCT-116 colon carcinoma cells.

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