Evaluation of copper chelation agents as anti-angiogenic therapy

Kevin Camphausen, Mary Sproull, Steve Tantama, Sandeep Sankineni, Tamalee Scott, Cynthia Ménard, C. Norman Coleman, Martin W. Brechbiel

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Pages (from-to)4287-4293
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume11
Issue number19
DOIs
StatePublished - Sep 15 2003

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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