Evaluation of copper chelation agents as anti-angiogenic therapy.

Abstract

The design, synthesis and evaluation of N,N',N"-tris(2-pyridylmethyl)-cis,cis-1,3,5,-triaminocyclohexane (tachpyr, 1) derivatives as novel anti-angiogenic agents were performed in an in vitro endothelial cell proliferation assay to assess their cytotoxicity and selectivity. The selective nature of the anti-angiogenic agents for human umbilical vein endothelial cells (Huvec) was compared to a normal fibroblast cell line and a human Glioma cell line to evaluate these compounds. N,N',N"-tris(2-mercaptoethyl)-cis,cis-1,3,5-triaminocyclohexane trihydrochloride (3b) was superior to tachpyr in terms of selectivity of its inhibitory activity toward the proliferation of Huvec compared to the fibroblast and human Glioma cell lines.

• Authors: Kevin Camphausen, Mary Sproull, Steve Tantama, Sandeep Sankineni, Tamalee Scott, Cynthia Ménard, C Norman Coleman, Martin W Brechbiel
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 11 Issue 19 Pg. 4287-93 (Sep 15 2003) ISSN: 0968-0896 [Print] England
• PMID: 12951159 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Angiogenesis Inhibitors
• Chelating Agents
• Cyclohexylamines
• Pyridines
• tachpyr
• Copper

Topics

• Angiogenesis Inhibitors (chemical synthesis, pharmacology, therapeutic use)
• Cell Division (drug effects)
• Cell Line
• Cell Line, Tumor
• Cells, Cultured
• Chelating Agents (chemical synthesis, pharmacology, therapeutic use)
• Copper (chemistry)
• Cyclohexylamines (chemical synthesis, pharmacology, therapeutic use)
• Dose-Response Relationship, Drug
• Drug Design
• Endothelial Cells (drug effects)
• Fibroblasts
• Glioma
• Humans
• Inhibitory Concentration 50
• Pyridines (chemical synthesis, pharmacology, therapeutic use)
• Umbilical Veins