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

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.

Graphical abstractTwo novel N-(2,4-dinitrophenylamine) derivatives containing 5-fluorouracil and hydroxyurea moieties were synthesized and their aerobic cytotoxicities toward HT-29 adenocarcinoma cell line with and without radiation in comparison to their components were evaluated.Figure optionsDownload full-size imageDownload as PowerPoint slide