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.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-11, Vol.14 (21), p.5343-5346
Hauptverfasser:	JOSE, Binoy, ONIKI, Yusuke, KATO, Tamaki, NISHINO, Norikazu, SUMIDA, Yuko, YOSHIDA, Minoru
Format:	Artikel
Sprache:	eng
Schlagworte:	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
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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