Heterocyclic ketones as inhibitors of histone deacetylase

Several heterocyclic ketones were investigated as potential inhibitors of histone deacetylase. Nanomolar inhibitors such as 22 and 25 were obtained, the anti-proliferative activity of which were shown to be mediated by HDAC inhibition. Structure–activity relationships of a novel series of histone de...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (22), p.3909-3913
Main Authors: Vasudevan, Anil, Ji, Zhiqin, Frey, Robin R., Wada, Carol K., Steinman, Douglas, Heyman, H.Robin, Guo, Yan, Curtin, Michael L., Guo, Jun, Li, Junling, Pease, Lori, Glaser, Keith B., Marcotte, Patrick A., Bouska, Jennifer J., Davidsen, Steven K., Michaelides, Michael R.
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General aspects
Heterocyclic Compounds - pharmacology
Histone Deacetylase Inhibitors
Ketones - chemistry
Ketones - pharmacology
Kinetics
Medical sciences
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:Several heterocyclic ketones were investigated as potential inhibitors of histone deacetylase. Nanomolar inhibitors such as 22 and 25 were obtained, the anti-proliferative activity of which were shown to be mediated by HDAC inhibition. Structure–activity relationships of a novel series of histone deacetylase inhibitors comprising electrophilic ketones are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.09.007