Fluorinated nucleoside analogs as anticancer and antiviral agents

What is it about?

Fluorinated nucleosides represent a significant class of chemotherapeutics widely used in the clinic. This review summarizes fluorination methods (including 18F-radiolabeling used in the synthesis of fluorine-containing nucleoside analogs), as well as clinical properties of FDA-approved and fluorinated nucleos(t)ide analogs in the clinical development.

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Why is it important?

We emphasize an important role that fluorine plays within many drug molecules imparting a variety of chemical and physical properties influencing molecular stability, solubility and target binding properties. We also outline current developments and strategies aiming to improve a clinical outcome of fluorinated nucleosides such as anticancer agent gemcitabine. We discuss recent developments in fluorine incorporation chemistry applied also in the field of 18F PET radiochemistry.