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 language | English (US) |
|---|---|
| Pages (from-to) | 4287-4293 |
| Number of pages | 7 |
| Journal | Bioorganic and Medicinal Chemistry |
| Volume | 11 |
| Issue number | 19 |
| DOIs | |
| State | Published - Sep 15 2003 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
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 journal › Article
}
TY - JOUR
T1 - Evaluation of copper chelation agents as anti-angiogenic therapy
AU - Camphausen, Kevin
AU - Sproull, Mary
AU - Tantama, Steve
AU - Sankineni, Sandeep
AU - Scott, Tamalee
AU - Ménard, Cynthia
AU - Coleman, C. Norman
AU - Brechbiel, Martin W.
PY - 2003/9/15
Y1 - 2003/9/15
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0041888242&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0041888242&partnerID=8YFLogxK
U2 - 10.1016/S0968-0896(03)00401-2
DO - 10.1016/S0968-0896(03)00401-2
M3 - Article
C2 - 12951159
AN - SCOPUS:0041888242
VL - 11
SP - 4287
EP - 4293
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 19
ER -