Preliminary evaluation of the cytotoxicity of a series of tris-2-aminoethylamine (Tren) based hexadentate heterocyclic donor agents.
Tachpyridine is a cytotoxic metal chelator with potential anti-tumor activity. The synthesis and evaluation of a set of derivatives of the related hexadentate heterocyclic donor agents tris-2-aminoethylamine (tren) and tris[N-(2-pyridylmethylene)-2-aminoethyl]amine (trenpyr) was performed to compare their cytotoxic activity to tachpyridine in HeLa tumor cells. Methyl groups were added to the pyridyl ring of trenpyr, and the effects of alkyl group substitution on cell survival were assessed. Profound cytotoxicity was observed and IC50 data were obtained in ascending order from those compounds substituted with a methyl group at the 3-, 4-, or 5-position and lastly by the 6-methyl derivative. These results suggest that analogous derivatives with substitution at the 3-position of the pyridyl ring deserve further exploration.
Torti
Suzy V
SV
Department of Biochemistry, The Comprehensive Cancer Center, Wake Forest University School of Medicine, Winston-Salem, NC, USA.
Ma
Rong
R
Venditto
Vincent J
VJ
Torti
Frank M
FM
Planalp
Roy P
RP
Brechbiel
Martin W
MW
D002470:Cell Survival / Q000187:drug effects; D002614:Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D005029:Ethylenediamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D002614:Chelating Agents; D005029:Ethylenediamines; D008024:Ligands; C099539:tris(2-aminoethyl)amine