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Page 1
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. Kotschy A, et al. Among authors: surgenor a. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.
Williamson DS, Parratt MJ, Bower JF, Moore JD, Richardson CM, Dokurno P, Cansfield AD, Francis GL, Hebdon RJ, Howes R, Jackson PS, Lockie AM, Murray JB, Nunns CL, Powles J, Robertson A, Surgenor AE, Torrance CJ. Williamson DS, et al. Among authors: surgenor ae. Bioorg Med Chem Lett. 2005 Feb 15;15(4):863-7. doi: 10.1016/j.bmcl.2004.12.073. Bioorg Med Chem Lett. 2005. PMID: 15686876
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.
Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ. Richardson CM, et al. Among authors: surgenor ae. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. doi: 10.1016/j.bmcl.2005.11.048. Epub 2005 Dec 1. Bioorg Med Chem Lett. 2006. PMID: 16325401
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.
Richardson CM, Nunns CL, Williamson DS, Parratt MJ, Dokurno P, Howes R, Borgognoni J, Drysdale MJ, Finch H, Hubbard RE, Jackson PS, Kierstan P, Lentzen G, Moore JD, Murray JB, Simmonite H, Surgenor AE, Torrance CJ. Richardson CM, et al. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3880-5. doi: 10.1016/j.bmcl.2007.04.110. Epub 2007 May 6. Bioorg Med Chem Lett. 2007. PMID: 17570665
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.
Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ. Williamson DS, et al. Among authors: surgenor ae. J Med Chem. 2009 Mar 26;52(6):1510-3. doi: 10.1021/jm801627a. J Med Chem. 2009. PMID: 19256508
Structure-guided design of alpha-amino acid-derived Pin1 inhibitors.
Potter AJ, Ray S, Gueritz L, Nunns CL, Bryant CJ, Scrace SF, Matassova N, Baker L, Dokurno P, Robinson DA, Surgenor AE, Davis B, Murray JB, Richardson CM, Moore JD. Potter AJ, et al. Among authors: surgenor ae. Bioorg Med Chem Lett. 2010 Jan 15;20(2):586-90. doi: 10.1016/j.bmcl.2009.11.090. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 19969456
Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution.
Potter A, Oldfield V, Nunns C, Fromont C, Ray S, Northfield CJ, Bryant CJ, Scrace SF, Robinson D, Matossova N, Baker L, Dokurno P, Surgenor AE, Davis B, Richardson CM, Murray JB, Moore JD. Potter A, et al. Among authors: surgenor ae. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6483-8. doi: 10.1016/j.bmcl.2010.09.063. Epub 2010 Sep 17. Bioorg Med Chem Lett. 2010. PMID: 20932746
Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity.
Macias AT, Williamson DS, Allen N, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Francis GL, Graham CJ, Howes R, Matassova N, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ. Macias AT, et al. Among authors: surgenor ae. J Med Chem. 2011 Jun 23;54(12):4034-41. doi: 10.1021/jm101625x. Epub 2011 May 20. J Med Chem. 2011. PMID: 21526763
35 results