Special properties of fluorine has been successfully exploited for the development of new and effective biochemical tools as well as therapeutic agents. Fluorinated congeners can also serve as excellent probes for the investigation of biochemical mechanisms. 19F-NMR can provide unique and powerful tools for the mechanistic investigations in chemical biology and 18F-PET has emerged as an important tool in drug development. This lecture presents recent progress in our research on the medicinal chemistry and drug discovery of (i) novel fluorotaxoids bearing trifluoromethoxy and difluoromethoxy groups at the C2-benzoate moiety, targeting microtubules, (ii) novel fluoro-analogs of vascular disrupting agent (VDA), combretastatin A-4, and (iii) novel fluorine-containing theranostic vitamin-drug conjugates, readily amenable to 18F-PET.

Strategic incorporation of fluorine into bioactive compounds for medicinal chemistry and drug discovery

253rd National Meeting (2017)

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