1. Academic Validation
  2. Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues

Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues

  • Bioorg Med Chem Lett. 2007 Nov 15;17(22):6142-6. doi: 10.1016/j.bmcl.2007.09.041.
Cédric Charrier 1 Joëlle Roche Jean-Pierre Gesson Philippe Bertrand
Affiliations

Affiliation

  • 1 Synthèse et Réactivité des Substances Naturelles, CNRS UMR 6514, Université de Poitiers, 40 Avenue du Recteur Pineau, Poitiers, France.
Abstract

New compounds derived from inhibitors of histone deacetylases (HDACs) have been synthesized and their antiproliferative activities towards non small lung Cancer cell line H661 evaluated. Their design is based on hybrids between indanones to limit conformational mobility and Other known HDAC inhibitors (SAHA, MS-275). The synthesis of these new derivatives was achieved by alkylation of appropriate indanones to introduce the side chain bearing a terminal ester group, the latter being a precursor of hydroxamic acid and aminobenzamide derivatives. These new analogues were found to be moderately active to inhibit H661 cell proliferation.

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