Highly Ligand Efficient and Selective N??2??(Thioethyl) picolinamide Histone Deacetylase Inhibitors Inspired by the Natural Product Psammaplin A

MGJ Baud, P Haus, T Leiser, FJ Meyer??Almes…

文献索引：Baud, Matthias G.J.; Haus, Patricia; Leiser, Thomas; Meyer-Almes, Franz-Josef; Fuchter, Matthew J. ChemMedChem, 2013 , vol. 8, # 1 p. 149 - 156

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被引用次数: 12

摘要

Abstract Novel picolinamide-based histone deacetylase (HDAC) inhibitors were developed, drawing inspiration from the natural product psammaplin A. We found that the HDAC potency and isoform selectivity provided by the oxime unit of psammaplin A could be reproduced by using carefully chosen heterocyclic frameworks. The resulting (hetero) aromatic amide based compounds displayed very high potency and isoform selectivity ...