Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia AE Tron, MA Belmonte, A Adam, BM Aquila, LH Boise, E Chiarparin, ... Nature communications 9 (1), 5341, 2018 | 472 | 2018 |
Designing novel building blocks is an overlooked strategy to improve compound quality FW Goldberg, JG Kettle, T Kogej, MWD Perry, NP Tomkinson Drug Discovery Today 20 (1), 11-17, 2015 | 207 | 2015 |
Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally … M Addie, P Ballard, D Buttar, C Crafter, G Currie, BR Davies, J Debreczeni, ... Journal of medicinal chemistry 56 (5), 2059-2073, 2013 | 197 | 2013 |
Synthesis of brevetoxin sub-units by sequential ring-closing metathesis and hydroboration J Stephen, JG Kettle Tetrahedron letters 38 (1), 123-126, 1997 | 180 | 1997 |
Enantioselective synthesis of medium-ring sub-units of brevetoxin A by ring-closing metathesis JS Clark, JG Kettle Tetrahedron letters 38 (1), 127-130, 1997 | 161 | 1997 |
Potent and selective inhibitors of MTH1 probe its role in cancer cell survival JG Kettle, H Alwan, M Bista, J Breed, NL Davies, K Eckersley, S Fillery, ... Journal of medicinal chemistry 59 (6), 2346-2361, 2016 | 155 | 2016 |
Small molecule binding sites on the Ras: SOS complex can be exploited for inhibition of Ras activation JJG Winter, M Anderson, K Blades, C Brassington, AL Breeze, C Chresta, ... Journal of medicinal chemistry 58 (5), 2265-2274, 2015 | 138 | 2015 |
Synthesis of sub-units of marine polycyclic ethers by ring-closing metathesis and hydroboration of enol ethers JS Clark, JG Kettle Tetrahedron 55 (27), 8231-8248, 1999 | 135 | 1999 |
Expanding medicinal chemistry space A Barker, JG Kettle, T Nowak, JE Pease Drug discovery today 18 (5-6), 298-304, 2013 | 124 | 2013 |
Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors A Baxter, S Brough, A Cooper, E Floettmann, S Foster, C Harding, J Kettle, ... Bioorganic & Medicinal Chemistry Letters 14 (11), 2817-2822, 2004 | 111 | 2004 |
Structure-based design of potent and selective inhibitors of the metabolic kinase PFKFB3 S Boyd, JL Brookfield, SE Critchlow, IA Cumming, NJ Curtis, J Debreczeni, ... Journal of medicinal chemistry 58 (8), 3611-3625, 2015 | 94 | 2015 |
Quinazoline derivatives as antitumor agents L Hennequin, J Kettle, M Pass, R Bradbury US Patent App. 10/494,388, 2005 | 86 | 2005 |
Novel 3-alkoxy-1H-pyrazolo [3, 4-d] pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors R Ducray, P Ballard, BC Barlaam, MD Hickinson, JG Kettle, DJ Ogilvie, ... Bioorganic & medicinal chemistry letters 18 (3), 959-962, 2008 | 85 | 2008 |
General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor FW Goldberg, JG Kettle, J Xiong, D Lin Tetrahedron 70 (37), 6613-6622, 2014 | 79 | 2014 |
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2, 4-bis-anilinopyrimidines C Bardelle, D Cross, S Davenport, JG Kettle, EJ Ko, AG Leach, A Mortlock, ... Bioorganic & medicinal chemistry letters 18 (9), 2776-2780, 2008 | 73 | 2008 |
A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr286, not Thr288 AL Ashford, D Oxley, J Kettle, K Hudson, S Guichard, SJ Cook, ... Biochemical Journal 457 (1), 43-56, 2014 | 72 | 2014 |
Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1 JG Kettle, A Åstrand, M Catley, NP Grimster, M Nilsson, Q Su, R Woessner Expert Opinion on Therapeutic Patents 27 (2), 127-143, 2017 | 71 | 2017 |
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT JG Kettle, S Brown, C Crafter, BR Davies, P Dudley, G Fairley, P Faulder, ... Journal of medicinal chemistry 55 (3), 1261-1273, 2012 | 68 | 2012 |
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C JG Kettle, SK Bagal, S Bickerton, MS Bodnarchuk, J Breed, RJ Carbajo, ... Journal of medicinal chemistry 63 (9), 4468-4483, 2020 | 66 | 2020 |
Orally bioavailable and blood–brain barrier-penetrating ATM inhibitor (AZ32) radiosensitizes intracranial gliomas in mice J Karlin, J Allen, SF Ahmad, G Hughes, V Sheridan, R Odedra, ... Molecular cancer therapeutics 17 (8), 1637-1647, 2018 | 64 | 2018 |