Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones

Cyclic tetrapeptides containing trifluoromethyl and pentafluoroethyl ketone as zinc binding functional group were synthesized as potent HDAC inhibitors. Evaluation by human HDAC inhibition assay and p21 promoter assay showed that these inhibitors are promising anticancer agents.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-11, Vol.14 (21), p.5343-5346
Main Authors: JOSE, Binoy, ONIKI, Yusuke, KATO, Tamaki, NISHINO, Norikazu, SUMIDA, Yuko, YOSHIDA, Minoru
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Binding Sites
Biological and medical sciences
Chromatography, High Pressure Liquid
Drug Stability
General aspects
Histone Deacetylase Inhibitors
Histone Deacetylases - chemistry
Humans
Ketones - chemical synthesis
Ketones - chemistry
Medical sciences
Peptides, Cyclic - chemical synthesis
Peptides, Cyclic - chemistry
Peptides, Cyclic - pharmacology
Pharmacology. Drug treatments
Promoter Regions, Genetic
Proto-Oncogene Proteins p21(ras) - genetics
Structure-Activity Relationship
Zinc - chemistry
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Description
Summary:Cyclic tetrapeptides containing trifluoromethyl and pentafluoroethyl ketone as zinc binding functional group were synthesized as potent HDAC inhibitors. Evaluation by human HDAC inhibition assay and p21 promoter assay showed that these inhibitors are promising anticancer agents.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.08.016