Jason Grant Kettle
Jason Grant Kettle
Principal Scientist, Medicinal Chemistry, Oncology iMED, AstraZeneca
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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
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
Synthesis of brevetoxin sub-units by sequential ring-closing metathesis and hydroboration
J Stephen, JG Kettle
Tetrahedron letters 38 (1), 123-126, 1997
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
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
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
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
Expanding medicinal chemistry space
A Barker, JG Kettle, T Nowak, JE Pease
Drug discovery today 18 (5-6), 298-304, 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
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
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
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
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
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
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
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
Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3, 5-bis substituted anilinopyrimidines
C Bardelle, T Coleman, D Cross, S Davenport, JG Kettle, EJ Ko, ...
Bioorganic & medicinal chemistry letters 18 (21), 5717-5721, 2008
Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket
P Ballard, RH Bradbury, CS Harris, LFA Hennequin, M Hickinson, ...
Bioorganic & medicinal chemistry letters 16 (6), 1633-1637, 2006
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
Quinazoline derivatives as antitumor agents
L Hennequin, J Kettle, M Pass, R Bradbury
US Patent App. 10/494,388, 2005
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