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

Binoy Jose; Yusuke Oniki; Tamaki Kato; Norikazu Nishino; Yuko Sumida; Minoru Yoshida

doi:10.1016/j.bmcl.2004.08.016

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

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5343-6. doi: 10.1016/j.bmcl.2004.08.016.

Authors

Binoy Jose¹, Yusuke Oniki, Tamaki Kato, Norikazu Nishino, Yuko Sumida, Minoru Yoshida

Affiliation

¹ CREST Research Project, Japan Science and Technology Agency, Saitama 332-0012, Japan.

PMID: 15454224
DOI: 10.1016/j.bmcl.2004.08.016

Abstract

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.

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Binding Sites
Chromatography, High Pressure Liquid
Drug Stability
Histone Deacetylase Inhibitors*
Histone Deacetylases / chemistry*
Humans
Ketones / chemical synthesis*
Ketones / chemistry
Peptides, Cyclic / chemical synthesis*
Peptides, Cyclic / chemistry
Peptides, Cyclic / pharmacology
Promoter Regions, Genetic
Proto-Oncogene Proteins p21(ras) / genetics
Structure-Activity Relationship
Zinc / chemistry

Substances

Antineoplastic Agents
Histone Deacetylase Inhibitors
Ketones
Peptides, Cyclic
Histone Deacetylases
HRAS protein, human
Proto-Oncogene Proteins p21(ras)
Zinc