2. Academic Validation
  3. Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors

Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors

  • Bioorg Med Chem Lett. 2007 Sep 1;17(17):4819-23. doi: 10.1016/j.bmcl.2007.06.067.
Lynda Loudni 1,  Joëlle Roche,  Vincent Potiron,  Jonathan Clarhaut,  Christian Bachmann,  Jean-Pierre Gesson,  Isabelle Tranoy-Opalinski
Affiliations

Affiliation

  • 1 Université de Poitiers, CNRS UMR 6514, SRSN, 40 Avenue du Recteur Pineau, 86022, Poitiers, France.
PMID: 17624773 DOI: 10.1016/j.bmcl.2007.06.067
Abstract

New histone deacetylase inhibitors have been synthesized and evaluated for their activity against non-small lung Cancer cell line H661. These compounds have been designed with diversely substituted 1,4-benzodiazepine-2,5-dione moieties as cyclic peptide mimic cap structures, and a hydroxamate side chain. Biological evaluations demonstrated that benzodiazepine-based HDACi bearing an aromatic substituent at the N1 position exhibited promising antiproliferative and HDAC-inhibitory activities.

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