ISSN:
0947-3440
Keywords:
2′-Deoxy-5-fluorouridine derivatives
;
Phosphotriester method
;
Liposomes
;
Antitumor agents
;
MIA PaCa 2 pancreas tumor cell line
;
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
The new amphiphilic dinucleoside phosphate, 2′-deoxy-5-fluorouridylyl-(3′→5′)-2′-deoxy-5-fluoro-N4-octadecylcytidine (4) was synthesized on a gram scale, using the phosphotriester method, starting from the cytostatic drug 2′-deoxy-5-fluorouridine (5FdU) and 2′-deoxy-5-fluoro-N4-octadecylcytidine (1d). In in vitro clonogenic growth assays using the human pancreatic adenocarcinoma cell line MIA PaCa 2, the amphiphilic dimer was significantly more effective than the parent monomeric 5FdU. The IC50 of the dimer was 10 μg/ml when applied as an aqueous solution and 12 μg/ml when given as a liposome dispersion, whereas with 5FdU the IC50 concentration was not reached within the concentration range used.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/jlac.199719970220
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