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Page 1
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Seal JT, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Foley J, Gordon L, Grandi P, Gray JRJ, Harrison LA, Kruger RG, Matteo JJ, McCabe MT, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Wyce A, Zhang XP, Demont EH. Seal JT, et al. Among authors: demont eh. J Med Chem. 2021 Aug 12;64(15):10772-10805. doi: 10.1021/acs.jmedchem.1c00365. Epub 2021 Jul 13. J Med Chem. 2021. PMID: 34255512
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Hawkins J, Hussain I, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Soleil V, Smith KJ, Stanway S, Stemp G, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G. Clarke B, et al. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1017-21. doi: 10.1016/j.bmcl.2007.12.019. Epub 2007 Dec 15. Bioorg Med Chem Lett. 2008. PMID: 18166458
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Charrier N, Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, Hawkins J, Howes C, Hubbard J, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3664-8. doi: 10.1016/j.bmcl.2009.03.165. Epub 2009 Apr 17. Bioorg Med Chem Lett. 2009. PMID: 19428244
Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.
Charrier N, Clarke B, Demont E, Dingwall C, Dunsdon R, Hawkins J, Hubbard J, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3669-73. doi: 10.1016/j.bmcl.2009.03.150. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19477642
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.
Demont EH, Andrews BI, Bit RA, Campbell CA, Cooke JW, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Haynes A, Holmes DS, Kumar U, Morse MA, Osborne GJ, Panchal T, Patel B, Perboni A, Taylor S, Watson R, Witherington J, Willis R. Demont EH, et al. ACS Med Chem Lett. 2011 Mar 24;2(6):444-9. doi: 10.1021/ml2000214. eCollection 2011 Jun 9. ACS Med Chem Lett. 2011. PMID: 24900328 Free PMC article.
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. Gosmini R, et al. Among authors: demont eh. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. J Med Chem. 2014. PMID: 25249180
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ. Demont EH, et al. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5. doi: 10.1021/ml5002932. eCollection 2014 Nov 13. ACS Med Chem Lett. 2014. PMID: 25408830 Free PMC article.
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Skidmore J, Heer J, Johnson CN, Norton D, Redshaw S, Sweeting J, Hurst D, Cridland A, Vesey D, Wall I, Ahmed M, Rivers D, Myatt J, Giblin G, Philpott K, Kumar U, Stevens A, Bit RA, Haynes A, Taylor S, Watson R, Witherington J, Demont E, Heightman TD. Skidmore J, et al. J Med Chem. 2014 Dec 26;57(24):10424-42. doi: 10.1021/jm5010336. Epub 2014 Dec 15. J Med Chem. 2014. PMID: 25431977
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.
Demont EH, Chung CW, Furze RC, Grandi P, Michon AM, Wellaway C, Barrett N, Bridges AM, Craggs PD, Diallo H, Dixon DP, Douault C, Emmons AJ, Jones EJ, Karamshi BV, Locke K, Mitchell DJ, Mouzon BH, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ, Bamborough P. Demont EH, et al. J Med Chem. 2015 Jul 23;58(14):5649-73. doi: 10.1021/acs.jmedchem.5b00772. Epub 2015 Jul 9. J Med Chem. 2015. PMID: 26155854
52 results