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Updated: Aug 6, 2026

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
Synthesis of rigid trichostatin A analogs as HDAC inhibitors
Cédric Charrier1, Philippe Bertrand, Jean-Pierre Gesson
1Laboratoire Synthèse et Réactivité des Substances Naturelles, UMR 6514, Université de Poitiers et CNRS, 40 Avenue du Recteur Pineau, 86022 Poitiers, France.
Abstract:
New inhibitors of histone deacetylase (HDAC) have been synthesized and evaluated for their activity toward non small lung cancer cell line H661. Their design is based on indanone (or tetralone) systems leading to trichostatin A (TSA) analogs with limited conformational mobility. Molecular modelization at the AM1 level revealed that the conformations of indane-based analogs and TSA bound to HDAC like protein are similar. The synthesis of these new analogs was achieved by alkylation of an appropriate indanone (or tetralone) to introduce the side chain bearing a terminal ester group, the latter being a precursor of hydroxamic acid and aminobenzamide derivatives. Hydroxamic acids with the TSA side chain were found to be the most active compounds and the presence of the dimethylamino group on the phenyl ring turned out to be essential to achieve low micromolar activities against H661 cancer cells.
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