期刊
CHEMMEDCHEM
卷 8, 期 1, 页码 149-156出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201200450
关键词
epigenetics; HDAC inhibitors; isoform selectivity; ligand design; psammaplin A
资金
- Association for International Cancer Research [08-0407]
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.
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