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

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 an...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2003-11, Vol.46 (23), p.4826-4829
Main Authors: Mai, Antonello, Massa, Silvio, Pezzi, Riccardo, Rotili, Dante, Loidl, Peter, Brosch, Gerald
Format: Article
Language:English
Subjects:
Amides - chemical synthesis
Amides - chemistry
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Biological and medical sciences
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
General aspects
Histone Deacetylase Inhibitors
Medical sciences
Pharmacology. Drug treatments
Propionates - chemical synthesis
Propionates - chemistry
Pyrroles - chemical synthesis
Pyrroles - chemistry
Structure-Activity Relationship
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm034167p