Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores – A cautionary disclosure. Issue 4 (15th February 2019) - Acton, Ben
Graphical abstract: Abstract: Fluorination of metabolic hotspots in a molecule is a common medicinal chemistry strategy to improve in vivo half-life and exposure and, generally, this strategy offers significant benefits. Here, we report the application of this strategy to a series of poly-ADP ribose glycohydrolase (PARG) inhibitors, resulting in unexpected in vivo toxicity which was attributed to this single-atom modification.