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15 results

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Page 1
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. Among authors: butlin rj. 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.
Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.
Brocklehurst KJ, Broo A, Butlin RJ, Brown HS, Clarke DS, Davidsson Ö, Goldberg K, Groombridge SD, Kelly EE, Leach A, McKerrecher D, O'Donnell C, Poucher S, Schofield P, Scott JS, Teague J, Westgate L, Wood MJ. Brocklehurst KJ, et al. Among authors: butlin rj. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7310-6. doi: 10.1016/j.bmcl.2011.10.033. Epub 2011 Oct 18. Bioorg Med Chem Lett. 2011. PMID: 22061639
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
McCoull W, Addie MS, Birch AM, Birtles S, Buckett LK, Butlin RJ, Bowker SS, Boyd S, Chapman S, Davies RD, Donald CS, Green CP, Jenner C, Kemmitt PD, Leach AG, Moody GC, Gutierrez PM, Newcombe NJ, Nowak T, Packer MJ, Plowright AT, Revill J, Schofield P, Sheldon C, Stokes S, Turnbull AV, Wang SJ, Whalley DP, Wood JM. McCoull W, et al. Among authors: butlin rj. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8. doi: 10.1016/j.bmcl.2012.04.117. Epub 2012 May 2. Bioorg Med Chem Lett. 2012. PMID: 22608962
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Barlind JG, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbull AV, Vinblad J. Barlind JG, et al. Among authors: butlin rj. J Med Chem. 2012 Dec 13;55(23):10610-29. doi: 10.1021/jm301296t. Epub 2012 Nov 21. J Med Chem. 2012. PMID: 23116186
Phenoxypropylamines: a new series of squalene synthase inhibitors.
Brown GR, Butlin RJ, Chapman S, Eakin MA, Foubister AJ, Freeman S, Griffiths D, Harrison PJ, Johnson MC, Mallion KB, et al. Brown GR, et al. Among authors: butlin rj. J Med Chem. 1995 Oct 13;38(21):4157-60. doi: 10.1021/jm00021a003. J Med Chem. 1995. PMID: 7473541 No abstract available.
Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules.
Luker T, Alcaraz L, Chohan KK, Blomberg N, Brown DS, Butlin RJ, Elebring T, Griffin AM, Guile S, St-Gallay S, Swahn BM, Swallow S, Waring MJ, Wenlock MC, Leeson PD. Luker T, et al. Among authors: butlin rj. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5673-9. doi: 10.1016/j.bmcl.2011.07.074. Epub 2011 Jul 27. Bioorg Med Chem Lett. 2011. PMID: 21852131
New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides.
Bradbury RH, Bath C, Butlin RJ, Dennis M, Heys C, Hunt SJ, James R, Mortlock AA, Sumner NF, Tang EK, Telford B, Whiting E, Wilson C. Bradbury RH, et al. Among authors: butlin rj. J Med Chem. 1997 Mar 14;40(6):996-1004. doi: 10.1021/jm9604585. J Med Chem. 1997. PMID: 9083490
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy.
McCoull W, Bailey A, Barton P, Birch AM, Brown AJ, Butler HS, Boyd S, Butlin RJ, Chappell B, Clarkson P, Collins S, Davies RM, Ertan A, Hammond CD, Holmes JL, Lenaghan C, Midha A, Morentin-Gutierrez P, Moore JE, Raubo P, Robb G. McCoull W, et al. Among authors: butlin rj. J Med Chem. 2017 Apr 13;60(7):3187-3197. doi: 10.1021/acs.jmedchem.7b00210. Epub 2017 Apr 4. J Med Chem. 2017. PMID: 28374589
Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.
Scott JS, Birch AM, Brocklehurst KJ, Broo A, Brown HS, Butlin RJ, Clarke DS, Davidsson O, Ertan A, Goldberg K, Groombridge SD, Hudson JA, Laber D, Leach AG, Macfaul PA, McKerrecher D, Pickup A, Schofield P, Svensson PH, Sörme P, Teague J. Scott JS, et al. Among authors: butlin rj. J Med Chem. 2012 Jun 14;55(11):5361-79. doi: 10.1021/jm300310c. Epub 2012 May 17. J Med Chem. 2012. PMID: 22545772
15 results