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Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores - A cautionary disclosure.
Acton, Ben; Small, Helen F; Smith, Kate M; McGonagle, Alison; Stowell, Alexandra I J; James, Dominic I; Hamilton, Niall M; Hamilton, Nicola; Hitchin, James R; Hutton, Colin P; Waddell, Ian D; Ogilvie, Donald J; Jordan, Allan M.
Afiliação
  • Acton B; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Small HF; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Smith KM; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • McGonagle A; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Stowell AIJ; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • James DI; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Hamilton NM; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Hamilton N; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Hitchin JR; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Hutton CP; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Waddell ID; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Ogilvie DJ; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK.
  • Jordan AM; Drug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UK. Electronic address: allan.jordan@cruk.manchester.ac.uk.
Bioorg Med Chem Lett ; 29(4): 560-562, 2019 02 15.
Article em En | MEDLINE | ID: mdl-30616904
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Microssomos Hepáticos / Ciclopropanos / Glicosídeo Hidrolases Idioma: En Ano de publicação: 2019 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Microssomos Hepáticos / Ciclopropanos / Glicosídeo Hidrolases Idioma: En Ano de publicação: 2019 Tipo de documento: Article