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Page 1
Structure-Based Exploration of Selectivity for ATM Inhibitors in Huntington's Disease.
Van de Poël A, Toledo-Sherman L, Breccia P, Cachope R, Bate JR, Angulo-Herrera I, Wishart G, Matthews KL, Martin SL, Peacock M, Barnard A, Cox HC, Jones G, McAllister G, Vater H, Esmieu W, Clissold C, Lamers M, Leonard P, Jarvis RE, Blackaby W, Eznarriaga M, Lazari O, Yates D, Rose M, Jang SW, Muñoz-Sanjuan I, Dominguez C. Van de Poël A, et al. Among authors: jones g. J Med Chem. 2021 Apr 22;64(8):5018-5036. doi: 10.1021/acs.jmedchem.1c00114. Epub 2021 Mar 30. J Med Chem. 2021. PMID: 33783225
The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Heffron TP, Heald RA, Ndubaku C, Wei B, Augistin M, Do S, Edgar K, Eigenbrot C, Friedman L, Gancia E, Jackson PS, Jones G, Kolesnikov A, Lee LB, Lesnick JD, Lewis C, McLean N, Mörtl M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Staben ST, Steinbacher S, Tsui V, Wallin J, Sampath D, Olivero AG. Heffron TP, et al. Among authors: jones g. J Med Chem. 2016 Feb 11;59(3):985-1002. doi: 10.1021/acs.jmedchem.5b01483. Epub 2016 Jan 20. J Med Chem. 2016. PMID: 26741947
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Chan BK, Seward E, Lainchbury M, Brewer TF, An L, Blench T, Cartwright MW, Chan GKY, Choo EF, Drummond J, Elliott RL, Gancia E, Gazzard L, Hu B, Jones GE, Luo X, Madin A, Malhotra S, Moffat JG, Pang J, Salphati L, Sneeringer CJ, Stivala CE, Wei B, Wang W, Wu P, Heffron TP. Chan BK, et al. Among authors: jones ge. ACS Med Chem Lett. 2021 Dec 8;13(1):84-91. doi: 10.1021/acsmedchemlett.1c00473. eCollection 2022 Jan 13. ACS Med Chem Lett. 2021. PMID: 35059127 Free PMC article.
Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.
Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Huang J, Jones GE, Sukmar SK, Spitzfaden C, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND. Miles TJ, et al. Among authors: jones ge. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5437-41. doi: 10.1016/j.bmcl.2013.07.013. Epub 2013 Jul 17. Bioorg Med Chem Lett. 2013. PMID: 23968823
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
Miles TJ, Axten JM, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Gallagher T, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Miller WH, Minthorn EA, Rittenhouse S, Seefeld M, Pearson N. Miles TJ, et al. Among authors: jones g. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7489-95. doi: 10.1016/j.bmcl.2011.09.117. Epub 2011 Oct 10. Bioorg Med Chem Lett. 2011. PMID: 22047689
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.
Staben ST, Ndubaku C, Blaquiere N, Belvin M, Bull RJ, Dudley D, Edgar K, Gray D, Heald R, Heffron TP, Jones GE, Jones M, Kolesnikov A, Lee L, Lesnick J, Lewis C, Murray J, McLean NJ, Nonomiya J, Olivero AG, Ord R, Pang J, Price S, Prior WW, Rouge L, Salphati L, Sampath D, Wallin J, Wang L, Wei B, Weismann C, Wu P. Staben ST, et al. Among authors: jones m, jones ge. Bioorg Med Chem Lett. 2013 May 1;23(9):2606-13. doi: 10.1016/j.bmcl.2013.02.102. Epub 2013 Mar 7. Bioorg Med Chem Lett. 2013. PMID: 23540645
Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.
Miles TJ, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Rittenhouse S, Xiang H, Pearson N. Miles TJ, et al. Among authors: jones g. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7483-8. doi: 10.1016/j.bmcl.2011.09.114. Epub 2011 Oct 10. Bioorg Med Chem Lett. 2011. PMID: 22030032
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.
Bromidge SM, Dabbs S, Davies DT, Duckworth DM, Forbes IT, Ham P, Jones GE, King FD, Saunders DV, Starr S, Thewlis KM, Wyman PA, Blaney FE, Naylor CB, Bailey F, Blackburn TP, Holland V, Kennett GA, Riley GJ, Wood MD. Bromidge SM, et al. Among authors: jones ge. J Med Chem. 1998 May 7;41(10):1598-612. doi: 10.1021/jm970741j. J Med Chem. 1998. PMID: 9572885
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.
Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Jones GE, Kusalakumari Sukmar SK, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND. Miles TJ, et al. Among authors: jones ge. Bioorg Med Chem Lett. 2016 May 15;26(10):2464-2469. doi: 10.1016/j.bmcl.2016.03.106. Epub 2016 Mar 31. Bioorg Med Chem Lett. 2016. PMID: 27055939
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.
Bromidge SM, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, Gaster LM, Ham P, Jones GE, King FD, Mulholland KR, Saunders DV, Wyman PA, Blaney FE, Clarke SE, Blackburn TP, Holland V, Kennett GA, Lightowler S, Middlemiss DN, Trail B, Riley GJ, Wood MD. Bromidge SM, et al. Among authors: jones ge. J Med Chem. 2000 Mar 23;43(6):1123-34. doi: 10.1021/jm990388c. J Med Chem. 2000. PMID: 10737744
7,238 results