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Fuchs, S.; Kapp, T.; Otto, H.; Schöneberg, T.; Franke, P.;
Gust, R.; Schlüter, A. D.
"A set of surface-modified dendrimers with potential application
as drug delivery vehicles: Synthesis, in vitro cytotoxicity, and intracellular
localization"
Chem. Eur. J. 2003, in press.
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| Keywords |
Dendrimers, synthesis, drug delivery, cytotoxicity, cellular uptake |
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| Abstract |
The synthesis, cytotoxicity, and behavior in cell culture of a new
set of first (G1) and second generation (G2) dendrimers is reported.
The surface functionality of these dendrimers has been varied to see
whether structrue/toxicity relations can be observed. The outermost
functional groups are amides which are decorated either with protons,
Boc or Cbz protecting groups, Boc protected or unprotected natural amino
acid resiues, ethylene diamine ligands, and/or dansyl fluoresecence
labels. The cytotoxicity was determined in vitro in concentration dependent
assays using the human MCF-7 breat cancer cell line. Cell uptake and
intracellular distribution was monitored by confocal fluorescence microscopy
after internalization of the dansyl labelled dendrimers by HeLa cells. |
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