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Page 1
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: stowell aij. 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.
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: stowell aij. 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
Discovery of potent inhibitors of the lysophospholipase autotaxin.
Shah P, Cheasty A, Foxton C, Raynham T, Farooq M, Gutierrez IF, Lejeune A, Pritchard M, Turnbull A, Pang L, Owen P, Boyd S, Stowell A, Jordan A, Hamilton NM, Hitchin JR, Stockley M, MacDonald E, Quesada MJ, Trivier E, Skeete J, Ovaa H, Moolenaar WH, Ryder H. Shah P, et al. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5403-5410. doi: 10.1016/j.bmcl.2016.10.036. Epub 2016 Oct 14. Bioorg Med Chem Lett. 2016. PMID: 27780639
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. F1000Res. 2016 May 26;5:1005. doi: 10.12688/f1000research.8724.2. eCollection 2016. F1000Res. 2016. PMID: 27429741 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. 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
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT. Pappalardi MB, et al. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor.
Gilmartin AG, Groy A, Gore ER, Atkins C, Long ER, Montoute MN, Wu Z, Halsey W, McNulty DE, Ennulat D, Rueda L, Pappalardi M, Kruger RG, McCabe MT, Raoof A, Butlin R, Stowell A, Cockerill M, Waddell I, Ogilvie D, Luengo J, Jordan A, Benowitz AB. Gilmartin AG, et al. Haematologica. 2021 Jul 1;106(7):1979-1987. doi: 10.3324/haematol.2020.248658. Haematologica. 2021. PMID: 32586904 Free PMC article.