Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand

Norikazu Nishino; Daisuke Yoshikawa; Louis A Watanabe; Tamaki Kato; Binoy Jose; Yasuhiko Komatsu; Yuko Sumida; Minoru Yoshida

doi:10.1016/j.bmcl.2004.03.018

Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand

Bioorg Med Chem Lett. 2004 May 17;14(10):2427-31. doi: 10.1016/j.bmcl.2004.03.018.

Authors

Norikazu Nishino¹, Daisuke Yoshikawa, Louis A Watanabe, Tamaki Kato, Binoy Jose, Yasuhiko Komatsu, Yuko Sumida, Minoru Yoshida

Affiliation

¹ Faculty of Engineering, Kyushu Institute of Technology, Kitakyushu 808-8550, Japan. nishino@life.kyutech.ac.jp

PMID: 15109626
DOI: 10.1016/j.bmcl.2004.03.018

Abstract

Cyclic tetrapeptide retrohydroxamic acids were prepared as histone deacetylase (HDAC) inhibitors and evaluated the inhibitory activity and found that they have potential as anticancer drugs.

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / pharmacology
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology
Histone Deacetylase Inhibitors*
Hydroxamic Acids / chemistry
Inhibitory Concentration 50
Ligands
Mice
Molecular Structure
Oligopeptides / chemical synthesis
Oligopeptides / pharmacology
Peptides, Cyclic / chemical synthesis*
Peptides, Cyclic / pharmacology*
Structure-Activity Relationship
Zinc / chemistry

Substances

Antineoplastic Agents
Enzyme Inhibitors
Histone Deacetylase Inhibitors
Hydroxamic Acids
Ligands
Oligopeptides
Peptides, Cyclic
Zinc