Extreme modulation properties of aromatic fluorine

Thorough examination of the current literature as well as publicly available databases allowed us to qualify aromatic fluorine as a unique modulator of biological properties of organic compounds. In some rare cases, introduction of fluorine increased biological activity 100,000 times and even higher. We have also identified several examples where aromatic fluorine substantially reduced biological activity. Selected individual cases of extreme modulation are presented and discussed in the paper.

Graphical abstractAromatic fluorine is a unique modulator of biological properties of organic compounds. In some rare cases, introduction of aromatic fluorine improved biological activity more than 100,000 times and even higher.Figure optionsDownload full-size imageDownload as PowerPoint slideResearch highlights▶ Introduction of fluorine can improve biological potency by 4–5 orders of magnitude. ▶ Modulation properties of aromatic fluorine are structure dependent. ▶ Cases of negative fluorine modulation were observed in terminal benzene rings.