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Nucleoside transport inhibitors: structure-activity relationships for pyrimido[5,4-d]pyrimidine derivatives that potentiate pemetrexed cytotoxicity in the presence of α1-acid glycoprotein.
Saravanan K, Barlow HC, Barton M, Calvert AH, Golding BT, Newell DR, Northen JS, Curtin NJ, Thomas HD, Griffin RJ. Saravanan K, et al. Among authors: thomas hd. J Med Chem. 2011 Mar 24;54(6):1847-59. doi: 10.1021/jm101493z. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366300
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction.
Chessari G, Hardcastle IR, Ahn JS, Anil B, Anscombe E, Bawn RH, Bevan LD, Blackburn TJ, Buck I, Cano C, Carbain B, Castro J, Cons B, Cully SJ, Endicott JA, Fazal L, Golding BT, Griffin RJ, Haggerty K, Harnor SJ, Hearn K, Hobson S, Holvey RS, Howard S, Jennings CE, Johnson CN, Lunec J, Miller DC, Newell DR, Noble MEM, Reeks J, Revill CH, Riedinger C, St Denis JD, Tamanini E, Thomas H, Thompson NT, Vinković M, Wedge SR, Williams PA, Wilsher NE, Zhang B, Zhao Y. Chessari G, et al. J Med Chem. 2021 Apr 8;64(7):4071-4088. doi: 10.1021/acs.jmedchem.0c02188. Epub 2021 Mar 24. J Med Chem. 2021. PMID: 33761253
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C. Myers SM, et al. Among authors: thomas hd. Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25. Eur J Med Chem. 2019. PMID: 31212132
Structure-guided design of purine-based probes for selective Nek2 inhibition.
Coxon CR, Wong C, Bayliss R, Boxall K, Carr KH, Fry AM, Hardcastle IR, Matheson CJ, Newell DR, Sivaprakasam M, Thomas H, Turner D, Yeoh S, Wang LZ, Griffin RJ, Golding BT, Cano C. Coxon CR, et al. Oncotarget. 2017 Mar 21;8(12):19089-19124. doi: 10.18632/oncotarget.13249. Oncotarget. 2017. PMID: 27833088 Free PMC article.
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C. Miller DC, et al. J Med Chem. 2022 May 12;65(9):6513-6540. doi: 10.1021/acs.jmedchem.1c01756. Epub 2022 Apr 25. J Med Chem. 2022. PMID: 35468293 Free PMC article.
Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361.
Calabrese CR, Almassy R, Barton S, Batey MA, Calvert AH, Canan-Koch S, Durkacz BW, Hostomsky Z, Kumpf RA, Kyle S, Li J, Maegley K, Newell DR, Notarianni E, Stratford IJ, Skalitzky D, Thomas HD, Wang LZ, Webber SE, Williams KJ, Curtin NJ. Calabrese CR, et al. Among authors: thomas hd. J Natl Cancer Inst. 2004 Jan 7;96(1):56-67. doi: 10.1093/jnci/djh005. J Natl Cancer Inst. 2004. PMID: 14709739
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
Tikhe JG, Webber SE, Hostomsky Z, Maegley KA, Ekkers A, Li J, Yu XH, Almassy RJ, Kumpf RA, Boritzki TJ, Zhang C, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR. Tikhe JG, et al. Among authors: thomas hd. J Med Chem. 2004 Oct 21;47(22):5467-81. doi: 10.1021/jm030513r. J Med Chem. 2004. PMID: 15481984
82 results