Reductive activation of 5-fluorodeoxyuridine prodrug possessing azide methyl group by hypoxic X-irradiation

We prepared a 5-fluorodeoxyuridine (5-FdUrd) derivative possessing azide methyl group (N3-FdUrd) as a novel radiation-activated prodrug. The parent antitumor agent, 5-FdUrd, was released efficiently from N3-FdUrd by hypoxic X-irradiation. On the other hand, the activation of N3-FdUrd was suppressed upon X-irradiation under aerobic conditions. A biological assay using A549 cells revealed that the cytotoxicity of N3-FdUrd was significantly enhanced by hypoxic X-irradiation.

Figure optionsDownload as PowerPoint slide