Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores – a cautionary disclosure.

Ben Acton, Helen Small, Kate Smith, Alison Mcgonagle, Alexandra Stowell, Dominic James, Niall Hamilton, Nicola Hamilton, James Hitchin, Colin Hutton, Ian Waddell, Donald Ogilvie, Allan Jordan

Research output: Contribution to journalArticlepeer-review


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.
Original languageEnglish
Pages (from-to)560-562
Number of pages2
JournalBioorganic and Medicinal Chemistry Letters
Issue number4
Early online date2 Jan 2019
Publication statusPublished - 15 Feb 2019


  • Ataxia
  • Animal welfare
  • Toxicophore

Research Beacons, Institutes and Platforms

  • Manchester Cancer Research Centre


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