Abstract

Several strategies used in the rational design and synthesis of fluorinated compounds as potential therapeutic agents are reviewed. Applications of fluorine substitution in empirical SAR studies for lead development also are discussed, along with the implications with respect to fluorine target interactions that can be derived from biological activities.

Keywords: fluorine substitution, 5-Fluorouracil (5-FU), T138067, Hydrolytic stability, cholesterol acyl transferas, monofluorination