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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. Among authors: waszkowycz b. 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
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. 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
Toxoflavins and deazaflavins as the first reported selective small molecule inhibitors of tyrosyl-DNA phosphodiesterase II.
Raoof A, Depledge P, Hamilton NM, Hamilton NS, Hitchin JR, Hopkins GV, Jordan AM, Maguire LA, McGonagle AE, Mould DP, Rushbrooke M, Small HF, Smith KM, Thomson GJ, Turlais F, Waddell ID, Waszkowycz B, Watson AJ, Ogilvie DJ. Raoof A, et al. Among authors: waszkowycz b. J Med Chem. 2013 Aug 22;56(16):6352-70. doi: 10.1021/jm400568p. Epub 2013 Jul 31. J Med Chem. 2013. PMID: 23859074
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: waszkowycz b. 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: waszkowycz b. 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.
Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia.
Maiques-Diaz A, Spencer GJ, Lynch JT, Ciceri F, Williams EL, Amaral FMR, Wiseman DH, Harris WJ, Li Y, Sahoo S, Hitchin JR, Mould DP, Fairweather EE, Waszkowycz B, Jordan AM, Smith DL, Somervaille TCP. Maiques-Diaz A, et al. Among authors: waszkowycz b. Cell Rep. 2018 Mar 27;22(13):3641-3659. doi: 10.1016/j.celrep.2018.03.012. Cell Rep. 2018. PMID: 29590629 Free PMC article.
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase.
Newton R, Waszkowycz B, Seewooruthun C, Burschowsky D, Richards M, Hitchin S, Begum H, Watson A, French E, Hamilton N, Jones S, Lin LY, Waddell I, Echalier A, Bayliss R, Jordan AM, Ogilvie D. Newton R, et al. Among authors: waszkowycz b. ACS Med Chem Lett. 2020 Feb 28;11(4):497-505. doi: 10.1021/acsmedchemlett.9b00615. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292556 Free PMC article.
First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib.
James DI, Smith KM, Jordan AM, Fairweather EE, Griffiths LA, Hamilton NS, Hitchin JR, Hutton CP, Jones S, Kelly P, McGonagle AE, Small H, Stowell AI, Tucker J, Waddell ID, Waszkowycz B, Ogilvie DJ. James DI, et al. Among authors: waszkowycz b. ACS Chem Biol. 2016 Nov 18;11(11):3179-3190. doi: 10.1021/acschembio.6b00609. Epub 2016 Oct 12. ACS Chem Biol. 2016. PMID: 27689388
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: waszkowycz b. F1000Res. 2016 May 26;5:1005. doi: 10.12688/f1000research.8724.2. eCollection 2016. F1000Res. 2016. PMID: 27429741 Free PMC article.
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.
Liebeschuetz JW, Jones SD, Morgan PJ, Murray CW, Rimmer AD, Roscoe JM, Waszkowycz B, Welsh PM, Wylie WA, Young SC, Martin H, Mahler J, Brady L, Wilkinson K. Liebeschuetz JW, et al. Among authors: waszkowycz b. J Med Chem. 2002 Mar 14;45(6):1221-32. doi: 10.1021/jm010944e. J Med Chem. 2002. PMID: 11881991
29 results