Synthesis of rigid trichostatin A analogs as HDAC inhibitors

C Charrier, P Bertrand, JP Gesson, J Roche

Index: Charrier, Cedric; Bertrand, Philippe; Gesson, Jean-Pierre; Roche, Joelle Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 20 p. 5339 - 5344

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Citation Number: 17

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 ...