The synthesis and application of functionalised quinuclidines

Autor: Hitchin, James Richard

Externí odkaz: http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.426128

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Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores – a cautionary disclosure

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

Publikováno v: Acton, B, Small, H, Smith, K, Mcgonagle, A, Stowell, A, James, D, Hamilton, N, Hamilton, N, Hitchin, J, Hutton, C, Waddell, I, Ogilvie, D & Jordan, A 2019, ' Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores – a cautionary disclosure. ', Bioorganic and Medicinal Chemistry Letters, vol. 29, no. 4, pp. 560-562 . https://doi.org/83288294

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 serie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______3818::cc53e563e40e23c76c0f8f5c720a4b1c
https://doi.org/83288294

Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells

Autor: Jones, Stuart, Ahmet, Jonathan, Ayton, Kelly, Ball, Matthew, Cockerill, Mark, Fairweather, Emma, Hamilton, Nicola, Harper, Paul, Hitchin, James, Jordan, Allan, Levy, Colin, Lopez, Ruth, Mckenzie, Edward, Packer, Martin, Plant, Darren, Simpson, Iain, Simpson, Peter, Sinclair, Ian, Somervaille, Tim C P, Small, Helen, Spencer, Gary J, Thomson, Graeme, Tonge, Michael, Waddell, Ian, Walsh, Jarrod, Waszkowycz, Bohdan, Wigglesworth, Mark, Wiseman, Daniel H, Ogilvie, Donald

Publikováno v: Jones, S, Ahmet, J, Ayton, K, Ball, M, Cockerill, M, Fairweather, E, Hamilton, N, Harper, P, Hitchin, J, Jordan, A, Levy, C, Lopez, R, Mckenzie, E, Packer, M, Plant, D, Simpson, I, Simpson, P, Sinclair, I, Somervaille, T C P, Small, H, Spencer, G J, Thomson, G, Tonge, M, Waddell, I, Walsh, J, Waszkowycz, B, Wigglesworth, M, Wiseman, D H & Ogilvie, D 2016, ' Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells ', Journal of Medicinal Chemistry, vol. 59, no. 24, pp. 11120-11137 . https://doi.org/10.1021/acs.jmedchem.6b01320

A collaborative high throughput screen of 1.35 million compounds against mutant (R132H) isocitrate dehydrogenase IDH1 led to the identification of a novel series of inhibitors. Elucidation of the bound ligand crystal structure showed that the inhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::5b4bc4cd83ea4460871147ff1b32c029
https://pubmed.ncbi.nlm.nih.gov/28002956

First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib

Autor: James, Dominic, Smith, Kate, Jordan, Allan, Fairweather, Emma, Griffiths, Louise, Hamilton, Nicola, Hitchin, James, Hutton, Colin, Jones, Stuart, Kelly, Paul, Mcgonagle, Alison, Small, Helen, Stowell, Alexandra, Tucker, Julie, Waddell, Ian, Waszkowycz, Bohdan, Ogilvie, Donald

Publikováno v: James, D, Smith, K, Jordan, A, Fairweather, E, Griffiths, L, Hamilton, N, Hitchin, J, Hutton, C, Jones, S, Kelly, P, Mcgonagle, A, Small, H, Stowell, A, Tucker, J, Waddell, I, Waszkowycz, B & Ogilvie, D 2016, ' First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib ', ACS chemical biology, vol. 11, no. 11, pp. 3179-3190 . https://doi.org/10.1021/acschembio.6b00609

The enzyme poly(ADP-ribose) glycohydrolase (PARG) performs a critical role in the repair of DNA single strand breaks (SSBs). However, a detailed understanding of its mechanism of action has been hampered by a lack of credible, cell-active chemical pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______3818::b05924aac0197d0dbba5b5df73123c0c
https://research.manchester.ac.uk/en/publications/978c6aff-f49a-4af1-822e-e2e59f99fd27