Fluorine-containing taxoid anticancer agents and their tumor-targeted drug delivery

This account presents our recent progress, in perspective, on the strategic incorporation of fluorine(s) for the development of taxoid-based tumor-targeted drug delivery systems. Through rational design, the unique nature of fluorine has been exploited to increase the potency and metabolic stability of taxoid anticancer agents as potent warheads, to validate linker release mechanisms, and to construct PET tracers to assess the biodistribution and efficacy of tumor-targeted drug conjugates.