Synthesis of rigid trichostatin A analogs as HDAC inhibitors

C Charrier, P Bertrand, JP Gesson, J Roche

文献索引：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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被引用次数: 17

摘要

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 ...