Discovery of (Aryloxopropenyl)pyrrolyl Hydroxyamides as Selective Inhibitors of Class IIa Histone Deacetylase Homologue HD1-A

Journal of Medicinal Chemistry
2003.0

Abstract

Chemical manipulations performed on aroyl pyrrolyl hydroxyamides, a new class of HDAC inhibitors previously reported by us, led to (aryloxopropenyl)pyrrolyl hydroxyamides 3a-g. Such compounds, showing better inhibitory activity against maize HD1-A than HD1-B (two homologues of mammalian class IIa and I HDACs, respectively), are the first class of IIa-selective inhibitors (fold selectivity: 7-78). They could be useful as tools for probing the biology of these enzymes and eventually as new anticancer agents with low toxicity.

Knowledge Graph

Similar Paper

Discovery of (Aryloxopropenyl)pyrrolyl Hydroxyamides as Selective Inhibitors of Class IIa Histone Deacetylase Homologue HD1-A
Journal of Medicinal Chemistry 2003.0
Class II (IIa)-Selective Histone Deacetylase Inhibitors. 1. Synthesis and Biological Evaluation of Novel (Aryloxopropenyl)pyrrolyl Hydroxyamides
Journal of Medicinal Chemistry 2005.0
Class II-selective histone deacetylase inhibitors. Part 2: Alignment-independent GRIND 3-D QSAR, homology and docking studies
European Journal of Medicinal Chemistry 2008.0
3-(4-Aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a New Class of Synthetic Histone Deacetylase Inhibitors
Journal of Medicinal Chemistry 2001.0
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2009.0
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a New Class of Synthetic Histone Deacetylase Inhibitors. 2. Effect of Pyrrole-C<sub>2</sub> and/or -C<sub>4</sub> Substitutions on Biological Activity
Journal of Medicinal Chemistry 2004.0
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a New Class of Synthetic Histone Deacetylase Inhibitors. 3. Discovery of Novel Lead Compounds through Structure-Based Drug Design and Docking Studies<sup>,</sup>
Journal of Medicinal Chemistry 2004.0
Synthesis and Biological Evaluation of 3-(4-Substituted-phenyl)-N-hydroxy-2-propenamides, a New Class of Histone Deacetylase Inhibitors
Journal of Medicinal Chemistry 2003.0
Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors
European Journal of Medicinal Chemistry 2014.0
2-Aroylindoles and 2-Aroylbenzofurans with N-Hydroxyacrylamide Substructures as a Novel Series of Rationally Designed Histone Deacetylase Inhibitors
Journal of Medicinal Chemistry 2007.0