2. Academic Validation
  3. Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression

Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression

  • J Med Chem. 2009 May 14;52(9):3112-5. doi: 10.1021/jm9002439.
Cédric Charrier 1,  Jonathan Clarhaut,  Jean-Pierre Gesson,  Guillermina Estiu,  Olaf Wiest,  Joëlle Roche,  Philippe Bertrand
Affiliations

Affiliation

  • 1 Laboratoire Synthèse et Réactivité des Substances Naturelles, Université de Poitiers, CNRS-UMR 6514, 40 Avenue du Recteur Pineau, Poitiers F-86022, France.
PMID: 19385600 DOI: 10.1021/jm9002439
Abstract

New benzofuranones were synthesized and evaluated toward NCI-H661 non-small cell lung Cancer cells. Benzamide derivatives possessed micromolar antiproliferative and histone deacetylase inhibitory activities and modulate histone H4 acetylation. Hydroxamic acids were found to be potent nanomolar antiproliferative agents and HDAC inhibitors. Computational analysis presented a rationale for the activities of the hydroxamate derivatives. Impact of the HDAC inhibition on the expression of E-cadherin and the SEMA3F tumor suppressor genes revealed new promising compounds for lung Cancer treatments.

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