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Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores - a cautionary disclosure
Acton, Ben Small, Helen F Smith, Kate M McGonagle, Alison E Stowell, Alexandra I J James, Dominic I Hamilton, Niall M Hamilton, Nicola S Hitchin, James R Hutton, Colin P
Acton, Ben
Small, Helen F
Smith, Kate M
McGonagle, Alison E
Stowell, Alexandra I J
James, Dominic I
Hamilton, Niall M
Hamilton, Nicola S
Hitchin, James R
Hutton, Colin P
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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.
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Date
2019
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Collections
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Type
Article
Citation
Acton B, Small HF, Smith KM, McGonagle A, Stowell AIJ, James DI, et al. Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores - a cautionary disclosure. Bioorg Med Chem Lett. 2019 Jan 2.