Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins

…, JJ Hollick, S Ronseaux, J Campbell, M Higgins…

文献索引：McCarthy, Anna R.; Pirrie, Lisa; Hollick, Jonathan J.; Ronseaux, Sebastien; Campbell, Johanna; Higgins, Maureen; Staples, Oliver D.; Tran, Fanny; Slawin, Alexandra M.Z.; Lain, Sonia; Westwood, Nicholas J. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 5 p. 1779 - 1793

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被引用次数: 25

摘要

The tenovins are small molecule inhibitors of the NAD+-dependent family of protein deacetylases known as the sirtuins. There remains considerable interest in inhibitors of this enzyme family due to possible applications in both cancer and neurodegenerative disease therapy. Through the synthesis of novel tenovin analogues, further insights into the structural requirements for activity against the sirtuins in vitro are provided. In addition, the activity of ...