Abstract
Inhibitors of histone deacetylases (HDACs) have been shown to induce differentiation and/or apoptosis of human tumor cells. Novel 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides have been prepared as a new class of HDAC inhibitors and evaluated for their antiproliferative activity and HDAC inhibitory activity. Incorporation of a 1,4-phenylene carboxamide linker, shown by 5, and a 4-(dimethylamino)phenyl or 4-(pyrrolidin-1-yl)phenyl group as a cap substructure generated highly potent hydroxamic acid-based HDAC inhibitors 5a and 5b.
Original language | English |
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Pages (from-to) | 5745-5751 |
Number of pages | 7 |
Journal | Journal of Medicinal Chemistry |
Volume | 46 |
Issue number | 26 |
DOIs | |
State | Published - 18 Dec 2003 |