psammaplin-a and picolinamide

psammaplin-a has been researched along with picolinamide* in 1 studies

Other Studies

1 other study(ies) available for psammaplin-a and picolinamide

Article	Year
Highly ligand efficient and selective N-2-(Thioethyl)picolinamide histone deacetylase inhibitors inspired by the natural product psammaplin A. ChemMedChem, 2013, Volume: 8, Issue:1 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 among the HDAC family, in addition to excellent ligand efficiency relative to previously reported HDAC inhibitors. In particular, the high HDAC1 isoform selectivity provided by the chloropyridine motif represents a valuable design criterion for the development of new lead compounds and chemical probes that target HDAC1. Topics: Amides; Disulfides; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Docking Simulation; Picolinic Acids; Protein Isoforms; Tyrosine	2013

Article

Year

Highly ligand efficient and selective N-2-(Thioethyl)picolinamide histone deacetylase inhibitors inspired by the natural product psammaplin A.

ChemMedChem, 2013, Volume: 8, Issue:1

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 among the HDAC family, in addition to excellent ligand efficiency relative to previously reported HDAC inhibitors. In particular, the high HDAC1 isoform selectivity provided by the chloropyridine motif represents a valuable design criterion for the development of new lead compounds and chemical probes that target HDAC1.

Topics: Amides; Disulfides; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Docking Simulation; Picolinic Acids; Protein Isoforms; Tyrosine

2013