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

M Bigioni, A Ettorre, P Felicetti, S Mauro, C Rossi…

Index: Bigioni, Mario; Ettorre, Alessandro; Felicetti, Patrizia; Mauro, Sandro; Rossi, Cristina; Maggi, Carlo Alberto; Marastoni, Elena; Binaschi, Monica; Parlani, Massimo; Fattori, Daniela Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 17 p. 5360 - 5362

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Citation Number: 8

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 ...