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 journalArticle

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
Externally publishedYes

Fingerprint

Endothelial cells
Chelation
Copper
Human Umbilical Vein Endothelial Cells
Cells
Fibroblasts
Glioma
Cell Line
Cell proliferation
Cytotoxicity
Assays
Therapeutics
Endothelial Cells
Cell Proliferation
Derivatives
1,3,5-triaminocyclohexane
tachpyr

ASJC Scopus subject areas

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

Cite this

Camphausen, K., Sproull, M., Tantama, S., Sankineni, S., Scott, T., Ménard, C., ... Brechbiel, M. W. (2003). Evaluation of copper chelation agents as anti-angiogenic therapy. Bioorganic and Medicinal Chemistry, 11(19), 4287-4293. https://doi.org/10.1016/S0968-0896(03)00401-2

Evaluation of copper chelation agents as anti-angiogenic therapy. / Camphausen, Kevin; Sproull, Mary; Tantama, Steve; Sankineni, Sandeep; Scott, Tamalee; Ménard, Cynthia; Coleman, C. Norman; Brechbiel, Martin W.

In: Bioorganic and Medicinal Chemistry, Vol. 11, No. 19, 15.09.2003, p. 4287-4293.

Research output: Contribution to journalArticle

Camphausen, K, Sproull, M, Tantama, S, Sankineni, S, Scott, T, Ménard, C, Coleman, CN & Brechbiel, MW 2003, 'Evaluation of copper chelation agents as anti-angiogenic therapy', Bioorganic and Medicinal Chemistry, vol. 11, no. 19, pp. 4287-4293. https://doi.org/10.1016/S0968-0896(03)00401-2
Camphausen K, Sproull M, Tantama S, Sankineni S, Scott T, Ménard C et al. Evaluation of copper chelation agents as anti-angiogenic therapy. Bioorganic and Medicinal Chemistry. 2003 Sep 15;11(19):4287-4293. https://doi.org/10.1016/S0968-0896(03)00401-2
Camphausen, Kevin ; Sproull, Mary ; Tantama, Steve ; Sankineni, Sandeep ; Scott, Tamalee ; Ménard, Cynthia ; Coleman, C. Norman ; Brechbiel, Martin W. / Evaluation of copper chelation agents as anti-angiogenic therapy. In: Bioorganic and Medicinal Chemistry. 2003 ; Vol. 11, No. 19. pp. 4287-4293.
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