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75 results

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Page 1
Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells.
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 TC, Small H, Spencer GJ, Thomson G, Tonge M, Waddell I, Walsh J, Waszkowycz B, Wigglesworth M, Wiseman DH, Ogilvie D. Jones S, et al. J Med Chem. 2016 Dec 22;59(24):11120-11137. doi: 10.1021/acs.jmedchem.6b01320. Epub 2016 Dec 5. J Med Chem. 2016. PMID: 28002956
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.
Newton R, Bowler KA, Burns EM, Chapman PJ, Fairweather EE, Fritzl SJR, Goldberg KM, Hamilton NM, Holt SV, Hopkins GV, Jones SD, Jordan AM, Lyons AJ, Nikki March H, McDonald NQ, Maguire LA, Mould DP, Purkiss AG, Small HF, Stowell AIJ, Thomson GJ, Waddell ID, Waszkowycz B, Watson AJ, Ogilvie DJ. Newton R, et al. Among authors: waddell id. Eur J Med Chem. 2016 Apr 13;112:20-32. doi: 10.1016/j.ejmech.2016.01.039. Epub 2016 Jan 29. Eur J Med Chem. 2016. PMID: 26874741 Free PMC article.
Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position.
Jordan AM, Begum H, Fairweather E, Fritzl S, Goldberg K, Hopkins GV, Hamilton NM, Lyons AJ, March HN, Newton R, Small HF, Vishwanath S, Waddell ID, Waszkowycz B, Watson AJ, Ogilvie DJ. Jordan AM, et al. Among authors: waddell id. Bioorg Med Chem Lett. 2016 Jun 1;26(11):2724-9. doi: 10.1016/j.bmcl.2016.03.100. Epub 2016 Mar 30. Bioorg Med Chem Lett. 2016. PMID: 27086121 Free PMC article.
Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade.
Watson AJ, Hopkins GV, Hitchin S, Begum H, Jones S, Jordan A, Holt S, March HN, Newton R, Small H, Stowell A, Waddell ID, Waszkowycz B, Ogilvie DJ. Watson AJ, et al. Among authors: waddell id. F1000Res. 2016 May 26;5:1005. doi: 10.12688/f1000research.8724.2. eCollection 2016. F1000Res. 2016. PMID: 27429741 Free PMC article.
Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides.
Waszkowycz B, Smith KM, McGonagle AE, Jordan AM, Acton B, Fairweather EE, Griffiths LA, Hamilton NM, Hamilton NS, Hitchin JR, Hutton CP, James DI, Jones CD, Jones S, Mould DP, Small HF, Stowell AIJ, Tucker JA, Waddell ID, Ogilvie DJ. Waszkowycz B, et al. Among authors: waddell id. J Med Chem. 2018 Dec 13;61(23):10767-10792. doi: 10.1021/acs.jmedchem.8b01407. Epub 2018 Nov 19. J Med Chem. 2018. PMID: 30403352
Novel steroid inhibitors of glucose 6-phosphate dehydrogenase.
Hamilton NM, Dawson M, Fairweather EE, Hamilton NS, Hitchin JR, James DI, Jones SD, Jordan AM, Lyons AJ, Small HF, Thomson GJ, Waddell ID, Ogilvie DJ. Hamilton NM, et al. Among authors: waddell id. J Med Chem. 2012 May 10;55(9):4431-45. doi: 10.1021/jm300317k. Epub 2012 Apr 27. J Med Chem. 2012. PMID: 22506561
75 results