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Bioorg Med Chem Lett. 2006 Dec 1;16(23):6034-8. Epub 2006 Sep 20.

Synthesis, aerobic cytotoxicity, and radiosensitizing activity of novel 2,4-dinitrophenylamine tethered 5-fluorouracil and hydroxyurea.

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  • 1Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14174, Iran. <>


Two novel dual functional agents, 3[3-(2,4-dinitro-phenylamino)-propyl]-5-fluoro-1H-pyrimidine-2,4-dione 7 and N-[3-(2,4-dinitro-phenylamino)-propoxy]urea 8, resulting from linkage of 2,4-dinitrophenylamine through three carbon atoms with 5-fluorouracil 5 and hydroxyurea 6, respectively, were prepared and their in vitro aerobic cytotoxicities in HT-29 cell line with and without radiation were determined. Compounds 7 and 8 unlike their components were not cytotoxic but showed radiosensitizing activity.

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