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Page 1
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Bradbury RH, Callis R, Carr GR, Chen H, Clark E, Feron L, Glossop S, Graham MA, Hattersley M, Jones C, Lamont SG, Ouvry G, Patel A, Patel J, Rabow AA, Roberts CA, Stokes S, Stratton N, Walker GE, Ward L, Whalley D, Whittaker D, Wrigley G, Waring MJ. Bradbury RH, et al. Among authors: graham ma. J Med Chem. 2016 Sep 8;59(17):7801-17. doi: 10.1021/acs.jmedchem.6b00070. Epub 2016 Aug 24. J Med Chem. 2016. PMID: 27528113
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Kettle JG, Ballard P, Bardelle C, Cockerill M, Colclough N, Critchlow SE, Debreczeni J, Fairley G, Fillery S, Graham MA, Goodwin L, Guichard S, Hudson K, Ward RA, Whittaker D. Kettle JG, et al. Among authors: graham ma. J Med Chem. 2015 Mar 26;58(6):2834-44. doi: 10.1021/acs.jmedchem.5b00098. Epub 2015 Mar 12. J Med Chem. 2015. PMID: 25738750
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.
Ward RA, Bethel P, Cook C, Davies E, Debreczeni JE, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Griffin N, Hanson L, Hopcroft P, Howard TD, Hudson J, James M, Jones CD, Jones CR, Lamont S, Lewis R, Lindsay N, Roberts K, Simpson I, St-Gallay S, Swallow S, Tang J, Tonge M, Wang Z, Zhai B. Ward RA, et al. Among authors: graham ma. J Med Chem. 2017 Apr 27;60(8):3438-3450. doi: 10.1021/acs.jmedchem.7b00267. Epub 2017 Apr 14. J Med Chem. 2017. PMID: 28376306
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).
Ward RA, Anderton MJ, Bethel P, Breed J, Cook C, Davies EJ, Dobson A, Dong Z, Fairley G, Farrington P, Feron L, Flemington V, Gibbons FD, Graham MA, Greenwood R, Hanson L, Hopcroft P, Howells R, Hudson J, James M, Jones CD, Jones CR, Li Y, Lamont S, Lewis R, Lindsay N, McCabe J, McGuire T, Rawlins P, Roberts K, Sandin L, Simpson I, Swallow S, Tang J, Tomkinson G, Tonge M, Wang Z, Zhai B. Ward RA, et al. Among authors: graham ma. J Med Chem. 2019 Dec 26;62(24):11004-11018. doi: 10.1021/acs.jmedchem.9b01295. Epub 2019 Nov 25. J Med Chem. 2019. PMID: 31710489
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Ward RA, Colclough N, Challinor M, Debreczeni JE, Eckersley K, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Hopcroft P, Howard TD, James M, Jones CD, Jones CR, Renshaw J, Roberts K, Snow L, Tonge M, Yeung K. Ward RA, et al. Among authors: graham ma. J Med Chem. 2015 Jun 11;58(11):4790-801. doi: 10.1021/acs.jmedchem.5b00466. Epub 2015 May 28. J Med Chem. 2015. PMID: 25977981
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode.
Finlay MR, Acton DG, Andrews DM, Barker AJ, Dennis M, Fisher E, Graham MA, Green CP, Heaton DW, Karoutchi G, Loddick SA, Morgentin R, Roberts A, Tucker JA, Weir HM. Finlay MR, et al. Among authors: graham ma. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4442-6. doi: 10.1016/j.bmcl.2008.06.027. Epub 2008 Jun 12. Bioorg Med Chem Lett. 2008. PMID: 18617397
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing.
Jones CD, Andrews DM, Barker AJ, Blades K, Daunt P, East S, Geh C, Graham MA, Johnson KM, Loddick SA, McFarland HM, McGregor A, Moss L, Rudge DA, Simpson PB, Swain ML, Tam KY, Tucker JA, Walker M. Jones CD, et al. Among authors: graham ma. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6369-73. doi: 10.1016/j.bmcl.2008.10.102. Epub 2008 Oct 25. Bioorg Med Chem Lett. 2008. PMID: 18996007
224 results