J. Kettle

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Data-mining patent literature for novel chemical reagents for use in medicinal chemistry design

Jason G. Kettle, Richard A. Ward, E. Griffen, 2010 .

Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.

Jon Read, Andrew G. Leach, Andrew G Leach, 2008, Bioorganic & medicinal chemistry letters.

Structure-based design and pharmacokinetic optimization of covalent allosteric inhibitors of the mutant GTPase KRASG12C.

Doyle J Cassar, J. Breed, D. Ogg, 2020, Journal of medicinal chemistry.

Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation.

Malcolm Anderson, Jason G Kettle, Alexander L Breeze, 2015, Journal of medicinal chemistry.

Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors.

Stuart Paine, John Unitt, J. Unitt, 2004, Bioorganic & medicinal chemistry letters.

Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.

Rhys D O Jones, S. Guichard, W. Shao, 2018, Journal of medicinal chemistry.

A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288).

S. Cook, D. Oxley, S. Guichard, 2014, The Biochemical journal.

Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors.

David M. Robinson, M. Waring, D. Ogg, 2020, Journal of the American Chemical Society.

Facile synthesis of 7-amino anilinoquinazolines via direct amination of the quinazoline core

J. Kettle, E. Williams, C. Harris, 2005 .

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2

N. Grimster, A. Åstrand, Magnus Nilsson, 2017, Expert opinion on therapeutic patents.

Discovery of (2R)-N-[3-[2-[(3-methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a potent and selective Janus Kinase 1 (JAK1) inhibitor.

C. Chuaqui, A. Ferguson, P. Lyne, 2020, Journal of medicinal chemistry.

Identification and optimization of a novel series of selective PIP5K inhibitors.

D. M. Andrews, N. Divecha, R. Rowlinson, 2021, Bioorganic & medicinal chemistry.

N-Benzylindole-2-carboxylic acids: potent functional antagonists of the CCR2b chemokine receptor.

A. Barker, D. Davies, J. Kettle, 2004, Bioorganic & medicinal chemistry letters.

Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.

Andrew G. Leach, Paul D. Johnson, R. Morgentin, 2006, Bioorganic & medicinal chemistry letters.

SYNTHESIS OF 1,2,3,4,5,7-HEXAHYDRO-6H-AZOCINO[4,3-b]INDOL-6-ONES AS INTERMEDIATES FOR THE SYNTHESIS OF APPARICINE

J. Joule, J. Kettle, D. Roberts, 2010 .

Covalent inhibitors of the GTPase KRASG12C: a review of the patent literature

Doyle J Cassar, J. Kettle, 2020, Expert opinion on therapeutic patents.

Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.

Paul D. Johnson, R. Morgentin, R. Bradbury, 2006, Bioorganic & medicinal chemistry letters.

AZD4625 is a Potent and Selective Inhibitor of KRASG12C

A. Chakraborty, S. Cosulich, E. Wigmore, 2022, Molecular cancer therapeutics.

Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.

J. Debreczeni, A. Turnbull, S. Degorce, 2015, Journal of medicinal chemistry.

Synthesis of a 5-alkoxypyrido[4,3-d]pyrimidin-4(3H)-one derivative via a regioselective Meisenheimer N-oxide rearrangement

P. Kenny, Paul G. Mwashimba, J. Kettle, 2004 .

Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.

Jon Read, Andrew G. Leach, Andrew G Leach, 2008, Bioorganic & medicinal chemistry letters.

Alkene-arene meta photocycloadditions with a four-carbon-atom tether: efficient approach toward the polycyclic ring systems of aphidicolin and stemodinone.

J. Steed, J. Kettle, A. Russell, 2005, Angewandte Chemie.

Designing novel building blocks is an overlooked strategy to improve compound quality.

Matthew W D Perry, Thierry Kogej, Frederick W Goldberg, 2015, Drug discovery today.

General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor

Jason G. Kettle, J. Kettle, Frederick W. Goldberg, 2014 .

5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.

Paul D. Johnson, R. Morgentin, R. Bradbury, 2005, Bioorganic & medicinal chemistry letters.

Enantioselective synthesis of medium-ring sub-units of brevetoxin A by ring-closing metathesis

J. S. Clark, J. Kettle, J. Clark, 1997 .

Diverse heterocyclic scaffolds as allosteric inhibitors of AKT.

Simon J Brown, B. Davies, J. Pink, 2012, Journal of medicinal chemistry.

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

J. A. Hendricks, David M. Wilson, S. Kazmirski, 2018, Nature Communications.

Synthesis of sub-units of marine polycyclic ethers by ring-closing metathesis and hydroboration of enol ethers

J. S. Clark, J. Kettle, J. Clark, 1999 .

Selective alkylation of a 6,7-dihydroxyquinazoline

L. Hennequin, J. Kettle, C. Harris, 2005 .

Facile synthesis of 3-alkoxyindoles via rhodium(II)-catalysed diazoindole O–H insertion reactions

J. Kettle, Shaun M. Fillery, A. Faull, 2000 .

Synthesis of brevetoxin sub-units by sequential ring-closing metathesis and hydroboration

J. S. Clark, J. Kettle, J. Clark, 1997 .

Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.

Doyle J Cassar, Nichola L. Davies, J. Breed, 2022, Journal of medicinal chemistry.

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

James S. Scott, B. Barlaam, R. Ducray, 2008, Bioorganic & medicinal chemistry letters.

Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

James S. Scott, B. Barlaam, R. Bradbury, 2007, Bioorganic & medicinal chemistry letters.

Novel 3‐Alkoxy‐1H‐pyrazolo[3,4‐d]pyrimidines as EGFR and erbB2 Receptor Tyrosine Kinase Inhibitors.

B. Barlaam, R. Ducray, P. Ballard, 2008 .

Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.

Peter Ballard, Jason G. Kettle, B. Barlaam, 2008, Bioorganic & medicinal chemistry letters.

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 bioavailable, potent inhibitor of Akt kinases.

Peter Ballard, Andrew G. Leach, Jason G Kettle, 2013, Journal of medicinal chemistry.

Kinase Inhibitors in Cancer

B. Aquila, A. Mortlock, J. Kettle, 2013 .

Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.

J. Kendrew, R. Bradbury, P. Ballard, 2006, Bioorganic & medicinal chemistry letters.

Selective Kinase Inhibitors in Cancer

A. Mortlock, D. Wilson, J. Kettle, 2017 .

Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors

Rhys D O Jones, Jerome T. Mettetal, David M. Wilson, 2020, Science Translational Medicine.

Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival.

Graeme Walker, Lisa Wissler, Jon Read, 2016, Journal of medicinal chemistry.

Standing on the shoulders of giants: a retrospective analysis of kinase drug discovery at AstraZeneca.

David M. Wilson, J. Kettle, 2016, Drug discovery today.

Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

N. Mukhopadhyay, I. Barrett, K. Valerie, 2018, Molecular Cancer Therapeutics.

Chemical Biology Approaches Confirm MCT4 as the Therapeutic Target of a Cellular Optimized Hit.

G. Lamont, M. P. Castaldi, Andrew X. Zhang, 2023, ACS chemical biology.

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1

N. Grimster, A. Åstrand, Magnus Nilsson, 2017, Expert opinion on therapeutic patents.

Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology.

G. Lamont, D. Buttar, S. Critchlow, 2022, Journal of medicinal chemistry.

The Pharmacokinetic–Pharmacodynamic (PKPD) Relationships of AZD3229, a Novel and Selective Inhibitor of KIT, in a Range of Mouse Xenograft Models of GIST

Rhys D O Jones, S. Guichard, W. Shao, 2020, Clinical Cancer Research.

Expanding medicinal chemistry space.

Thorsten Nowak, Jason G Kettle, Andy Barker, 2013, Drug discovery today.

Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.

C. Chuaqui, A. Ferguson, P. Lyne, 2018, Journal of medicinal chemistry.

Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205

C. Chuaqui, P. Lyne, N. Grimster, 2017 .

Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.

D. Cross, B. Barlaam, R. Ducray, 2011, Bioorganic & medicinal chemistry letters.

Synthesis of a 5-alkoxypyrido[3,4-d]pyrimidin-4(3H)-one derivative via directed ortho-metallation of a pyridine analogue

Paul D. Johnson, J. Kettle, Allan P. Dishington, 2004 .

Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.

Mark Cockerill, J. Debreczeni, S. Guichard, 2015, Journal of medicinal chemistry.

Drugging the undruggable: a computational chemist's view of KRASG12C.

Michael S Bodnarchuk, Jason G Kettle, Graeme Robb, 2021, RSC medicinal chemistry.

Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.

Doyle J Cassar, Nichola L. Davies, J. Breed, 2023, Journal of medicinal chemistry.

Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.

B. Barlaam, R. Bradbury, P. Ballard, 2013, ACS medicinal chemistry letters.

Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization.

N. Grimster, Qibin Su, M. Lepistö, 2023, Journal of medicinal chemistry.

Systematic enumeration of heteroaromatic ring systems as reagents for use in medicinal chemistry.

Jason G Kettle, Richard A Ward, R. Ward, 2011, Journal of medicinal chemistry.

Vinylpyridine as a Tunable Covalent Warhead Targeting C797 in EGFR

E. Evertsson, J. Kettle, A. Argyrou, 2024, ACS Medicinal Chemistry Letters.

Abstract DDT01-02: AZD5991: A potent and selective macrocyclic inhibitor of Mcl-1 for treatment of hematologic cancers

S. Kazmirski, J. Tyner, D. Hargreaves, 2017 .