Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 66, Issue -, Pages 56-68Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.05.017
Keywords
HDAC inhibitors; 1,4-Benzodiazepine; Antiproliferative activity; Apoptosis; Enantioselectivity
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Funding
- MUR (PRIN) [200606139]
- University of Florence
- Ente Cassa di Risparmio di Firenze [726/2005]
- AIL (Associazione Italiana contro le Leucemie Linfomi e Mieloma, Firenze)
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A series of new histone deacetylase inhibitors were designed and synthesized based on hybridization between SAHA or oxamflatin and 5-phenyl-1,4-benzodiazepines. The compounds were tested for their enzyme inhibitory activity on HeLa nuclear extracts, and on human recombinant HDAC1 and HDAC6. Antiproliferative activity was tested on different cancer cells types, while proapoptotic activity was primarily tested on NB4 cells. The compounds showed IC50 values similar to those of SAHA. Compound (S)-8 displayed interesting activity against hematological and solid malignancies. (C) 2013 Elsevier Masson SAS. All rights reserved.
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