Radiolabeling and in vitro evaluation of a new 5-fluorouracil derivative with cell culture studies

The clinical impact and accessibility of Tc-99m tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple, and easy labeling process and radiopharmaceuticals. 5-Fluorouracil is an antitumor drug, which has played an important role for the treatment of breast carcinoma. In the present study, a new derivative of 5-Fluorouracil was synthesized as (1-[{1 '-(1 ''-deoxy-2 '',3 '':4 '',5 ''-di-O-isopropylidene-beta-D-fructopyranose-1 ''-yl)-1 ' H-1 ',2 ', 3 '-triazol-4 '-yl}methyl]-5-fluorouracil) (E) and radiolabeled with Tc-99m. It was analyzed by radio thin layer chromatography for quality control and stability. The radiolabeled complex was subjected to in vitro cell-binding studies to determine healthy and cancer cell affinity using HaCaT and MCF-7 cells, respectively. In addition, in vitro cytotoxicity studies of compound E were performed with HaCaT and MCF-5 cells. The radiochemical purity of the [Tc-99m]TcE was found to be higher than 90% at room temperature up to 6 hours. The radiolabeled complex showed higher specific binding to MCF-7 cells than HaCaT cells. IC50 values of E were found 31.5 +/- 3.4 mu M and 20.7 +/- 2.77 mu M for MCF-7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with Tc-99m has selective for breast cancer cells.