Abstract
Structural and biological properties of 5-fluorouracil (FU) bound zinc(II)–cyclen complex (FU––ZnL2+, L = cyclen; 1,4,7,10-tetrazacyclododecane) were studied in to develop an anticancer drug candidate. The complex formation was analyzed by X-ray crystallography and pH-titration study, and the anticancer activity was investigated by cytotoxicity examination against HL-60 cells. The crystal structure revealed that FU– and ZnL+ form the complex with 1:1 stoichiometry. The pH titration study proved that FU– has a strong affinity to ZnL+ at the physiological pH range (6.5–9.0). The IC50 values of FU––ZnL2+ against HL-60 cells growth was 132 μM in a quantitating cellular ATP levels. These results provide the basis for designing novel anticancer drug complexes and controlling FU release.
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