The incorporation of covalent fluorine has been widely used as an effective
strategy in medicinal chemistry for drug discovery. The introduction of fluorine into a
molecule can significantly influence conformation, lipophilicity, pKa, metabolism, and
pharmacokinetic properties. In 1955, the first fluorinated drug fludrocortisone has been
approved in the market for the treatment of the adrenogenital syndrome, postural
hypotension, and adrenal insufficiency. Since then, 218 small-molecule drugs with at
least one fluorine atom have been launched by U.S. FDA by the end of 2018.
Therefore, this chapter is expected to summarize the fluorine-containing natural
products in clinical development to the medicinal chemistry community.
Keywords: Antiproliferative, Antiviral, Anti-inflammatory, Clinical
Development, Drug Discovery, Fluorinated Drug, Medicinal Chemistry, Natural
Product, Nucleosides, Small-molecule, Steroids.
