Literature DB >> 17624773

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

Lynda Loudni1, Joëlle Roche, Vincent Potiron, Jonathan Clarhaut, Christian Bachmann, Jean-Pierre Gesson, Isabelle Tranoy-Opalinski.   

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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Year:  2007        PMID: 17624773     DOI: 10.1016/j.bmcl.2007.06.067

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  1,4-Thienodiazepine-2,5-diones via MCR (II): scaffold hopping by Gewald and Ugi-deprotection-cyclization strategy.

Authors:  Yijun Huang; Alexander Dömling
Journal:  Chem Biol Drug Des       Date:  2010-06-09       Impact factor: 2.817

Review 2.  Privileged diazepine compounds and their emergence as bromodomain inhibitors.

Authors:  Steven G Smith; Roberto Sanchez; Ming-Ming Zhou
Journal:  Chem Biol       Date:  2014-04-17

3.  Convergent synthesis of 13N-labelled Peptidic structures using aqueous [13N]NH3.

Authors:  Julia E Blower; Samuel F Cousin; Antony D Gee
Journal:  EJNMMI Radiopharm Chem       Date:  2017-12-19
  3 in total

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