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dc.contributor.authorActon, Ben
dc.contributor.authorSmall, Helen F
dc.contributor.authorSmith, Kate M
dc.contributor.authorMcGonagle, Alison E
dc.contributor.authorStowell, Alexandra I J
dc.contributor.authorJames, Dominic I
dc.contributor.authorHamilton, Niall M
dc.contributor.authorHamilton, Nicola S
dc.contributor.authorHitchin, James R
dc.contributor.authorHutton, Colin P
dc.contributor.authorWaddell, Ian D
dc.contributor.authorOgilvie, Donald J
dc.contributor.authorJordan, Allan M
dc.date.accessioned2019-02-08T15:20:10Z
dc.date.available2019-02-08T15:20:10Z
dc.date.issued2019en
dc.identifier.citationActon 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.en
dc.identifier.pmid30616904en
dc.identifier.doi10.1016/j.bmcl.2018.12.066en
dc.identifier.urihttp://hdl.handle.net/10541/621540
dc.description.abstractFluorination 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.en
dc.language.isoenen
dc.relation.urlhttps://dx.doi.org/10.1016/j.bmcl.2018.12.066en
dc.titleFluoromethylcyclopropylamine derivatives as potential in vivo toxicophores - a cautionary disclosureen
dc.typeArticleen
dc.contributor.departmentDrug Discovery Unit, Cancer Research UK Manchester Institute, The University of Manchester, Alderley Park, Macclesfield SK10 4TG, UKen
dc.identifier.journalBioorganic and Medicinal Chemistry Lettersen
dc.description.noteen]


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