Structural characterization of 5-fluorouracil & piperazine new solid forms and evaluation of their antitumor activity

摘要: Abstract A salt (FP–S) and two co-crystals (FP–C1 FP-C2) of fluorouracil (FU) with piperazine (PZ) were investigated in terms bioavailability their effect on endothelial cells. From structural point view, the best stability was observed for FP-C2 sample obtained by storage FP-C1 under extreme conditions temperature humidity. This result explained strong intermolecular interactions between 5-fluorouracil, water, as denoted crystallographic analysis form. Dissolution measurements water indicate that most soluble form is salt, a dissolution rate about 3 times greater than pure compound, while solubility decreases compared to FU. Toxicity antitumoral synthesized compounds checked three different cell lines: normal cells (HUVEC cells) tumor (DLD-1 HT29, both colorectal adenocarcinoma) cytotoxicity MTT assay proliferation assay. It has been found exerts selective cytotoxic HT29 cells DLD-1 cells contrast line resistance. For FU FP-S tumoral similar. The comparative study forms shows antitumor response co-crystal forms.