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1

Structure-based design and pharmacokinetic optimization of covalent allosteric inhibitors of the mutant GTPase KRAS G12C

Kettle, Jason Grant, Bagal, Sharan, Bickerton, Sue, Bodnarchuk, Michael Steven, Breed, Jason, Carbajo, Rodrigo J., Cassar, Doyle, Chakraborty, Atanu, Cosulich, Sabina, Cumming, Iain, Davies, Michael,

Journal:

Journal of Medicinal Chemistry

Year:

2020

Language:

english

File:

PDF, 1.12 MB

english, 2020

2

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

Catherine Bardelle, Darren Cross, Sara Davenport, Jason G. Kettle, Eun Jung Ko, Andrew G. Leach, Andrew Mortlock, Jon Read, Nicola J. Roberts, Peter Robins, Emma J. Williams

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 356 KB

english, 2008

3

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

Kettle, Jason G., Åstrand, Annika, Catley, Matthew, Grimster, Neil P., Nilsson, Magnus, Su, Qibin, Woessner, Richard

Journal:

Expert Opinion on Therapeutic Patents

Year:

2016

Language:

english

File:

PDF, 780 KB

english, 2016

4

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

Kettle, Jason G., Åstrand, Annika, Catley, Matthew, Grimster, Neil P., Nilsson, Magnus, Su, Qibin, Woessner, Richard

Journal:

Expert Opinion on Therapeutic Patents

Year:

2016

Language:

english

File:

PDF, 777 KB

english, 2016

5

Covalent inhibitors of the GTPase KRAS G12C : a review of the patent literature

Kettle, Jason G., Cassar, Doyle J.

Journal:

Expert Opinion on Therapeutic Patents

Year:

2020

File:

PDF, 2.17 MB

2020

6

Alkene–Arene meta Photocycloadditions with a Four-Carbon-Atom Tether: Efficient Approach toward the Polycyclic Ring Systems of Aphidicolin and Stemodinone

Joseph W. Boyd, Nicola Greaves, Jason Kettle, Andrew T. Russell, Jonathan W. Steed

Journal:

Angewandte Chemie

Year:

2005

Language:

english

File:

PDF, 115 KB

english, 2005

7

Alkene–Arene meta Photocycloadditions with a Four-Carbon-Atom Tether: Efficient Approach toward the Polycyclic Ring Systems of Aphidicolin and Stemodinone

Joseph W. Boyd, Nicola Greaves, Jason Kettle, Andrew T. Russell, Jonathan W. Steed

Journal:

Angewandte Chemie International Edition

Year:

2005

Language:

english

File:

PDF, 115 KB

english, 2005

8

ChemInform Abstract: Synthesis of Subunits of Marine Polycyclic Ethers by Ring-Closing Metathesis and Hydroboration of Enol Ethers.

J. Stephen Clark, Jason G. Kettle

Journal:

Year:

1999

File:

PDF, 31 KB

1999

9

ChemInform Abstract: Facile Synthesis of 3-Alkoxyindoles via Rhodium(II)-Catalyzed Diazoindole O—H Insertion Reactions.

Jason G. Kettle, Alan W. Faull, Shaun M. Fillery, Anthony P. Flynn, Marcus A. Hoyle, Julian A. Hudson

Journal:

Year:

2000

File:

PDF, 30 KB

2000

10

N-Benzylindole-2-carboxylic Acids: Potent Functional Antagonists of the CCR2b Chemokine Receptor.

Jason G. Kettle, Alan W. Faull, Andy J. Barker, D. Huw Davies, Michael A. Stone

Journal:

Year:

2004

File:

PDF, 81 KB

2004

11

Facile Synthesis of 7-Amino Anilinoquinazolines via Direct Amination of the Quinazoline Core.

Craig S. Harris, Jason G. Kettle, Emma J. Williams

Journal:

Year:

2006

File:

PDF, 24 KB

2006

12

ChemInform Abstract: Synthesis of 1,2,3,4,5,7-Hexahydro-6H-azocino[4,3-b]indol-6-ones as Intermediates for the Synthesis of Apparicine.

Jason G. Kettle, David Roberts, John A. Joule

Journal:

Year:

2011

File:

PDF, 38 KB

2011

13

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

Peter Ballard, Robert H. Bradbury, Craig S. Harris, Laurent F.A. Hennequin, Mark Hickinson, Jason G. Kettle, Jane Kendrew, Teresa Klinowska, Donald J. Ogilvie, Stuart E. Pearson, Emma J. Williams, Ing

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 136 KB

english, 2006

14

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

Bernard Barlaam, Peter Ballard, Robert H. Bradbury, Richard Ducray, Hervé Germain, D. Mark Hickinson, Kevin Hudson, Jason G. Kettle, Teresa Klinowska, Françoise Magnien, Donald J. Ogilvie, Annie Olivi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 134 KB

english, 2008

15

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

Jason G. Kettle, Alan W. Faull, Andy J. Barker, D.Huw Davies, Michael A. Stone

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 160 KB

english, 2004

16

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

Andrew Baxter, Steve Brough, Anne Cooper, Eike Floettmann, Steve Foster, Christine Harding, Jason Kettle, Tom McInally, Craig Martin, Michelle Mobbs, Maurice Needham, Pete Newham, Stuart Paine, Steve

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 385 KB

english, 2004

17

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

Peter Ballard, Robert H. Bradbury, Laurent F.A. Hennequin, D. Mark Hickinson, Paul D. Johnson, Jason G. Kettle, Teresa Klinowska, Remy Morgentin, Donald J. Ogilvie, Annie Olivier

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2005

Language:

english

File:

PDF, 219 KB

english, 2005

18

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

Peter Ballard, Robert H. Bradbury, Craig S. Harris, Laurent F.A. Hennequin, Mark Hickinson, Paul D. Johnson, Jason G. Kettle, Teresa Klinowska, Andrew G. Leach, Remy Morgentin, Martin Pass, Donald J.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 245 KB

english, 2006

19

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

Peter Ballard, Bernard C. Barlaam, Robert H. Bradbury, Allan Dishington, Laurent F.A. Hennequin, D. Mark Hickinson, Ian M. Hollingsworth, Jason G. Kettle, Teresa Klinowska, Donald J. Ogilvie, Stuart E

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2007

Language:

english

File:

PDF, 143 KB

english, 2007

20

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

Richard Ducray, Peter Ballard, Bernard C. Barlaam, Mark D. Hickinson, Jason G. Kettle, Donald J. Ogilvie, Catherine B. Trigwell

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 129 KB

english, 2008

21

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

Catherine Bardelle, Tanya Coleman, Darren Cross, Sara Davenport, Jason G. Kettle, Eun Jung Ko, Andrew G. Leach, Andrew Mortlock, Jon Read, Nicola J. Roberts, Peter Robins, Emma J. Williams

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 348 KB

english, 2008

22

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

Bernard Barlaam, Richard Ducray, Christine Lambert-van der Brempt, Patrick Plé, Catherine Bardelle, Nigel Brooks, Tanya Coleman, Darren Cross, Jason G. Kettle, Jon Read

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 353 KB

english, 2011

23

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

Emma J. Williams, Peter W. Kenny, Jason G. Kettle, Paul G. Mwashimba

Journal:

Tetrahedron Letters

Year:

2004

Language:

english

File:

PDF, 270 KB

english, 2004

24

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

Allan P. Dishington, Paul D. Johnson, Jason G. Kettle

Journal:

Tetrahedron Letters

Year:

2004

Language:

english

File:

PDF, 243 KB

english, 2004

25

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

Craig S. Harris, Jason G. Kettle, Emma J. Williams

Journal:

Tetrahedron Letters

Year:

2005

Language:

english

File:

PDF, 108 KB

english, 2005

26

Selective alkylation of a 6,7-dihydroxyquinazoline

Craig S. Harris, Laurent F. Hennequin, Jason G. Kettle, Olivier A. Willerval

Journal:

Tetrahedron Letters

Year:

2005

Language:

english

File:

PDF, 115 KB

english, 2005

27

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

J. Stephen Clark, Jason G. Kettle

Journal:

Tetrahedron Letters

Year:

1997

Language:

english

File:

PDF, 224 KB

english, 1997

28

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

J Stephen^Clark, Jason G Kettle

Journal:

Tetrahedron Letters

Year:

1997

Language:

english

File:

PDF, 237 KB

english, 1997

29

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

J. Stephen Clark, Jason G. Kettle

Journal:

Year:

1999

Language:

english

File:

PDF, 1.43 MB

english, 1999

30

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

Jason G Kettle, Alan W Faull, Shaun M Fillery, Anthony P Flynn, Marcus A Hoyle, Julian A Hudson

Journal:

Tetrahedron Letters

Year:

2000

Language:

english

File:

PDF, 112 KB

english, 2000

31

Systematic Enumeration of Heteroaromatic Ring Systems as Reagents for Use in Medicinal Chemistry

Ward, Richard A., Kettle, Jason G.

Journal:

Journal of Medicinal Chemistry

Year:

2011

Language:

english

File:

PDF, 1.01 MB

english, 2011

32

In vitro pharmacological profiles of kinase inhibitors: Comparison with other pharmaceuticals

Richard W.A. Luke, Mike G. Rolf, Rob H. Bradbury, Ed J. Griffen, Neil J. Hales, Jason Kettle, Andrew P. Thomas, Joanne Bowes, Jean-Pierre Valentin, Andy J. Barker

Journal:

Journal of Pharmacological and Toxicological Methods

Year:

2009

Language:

english

File:

PDF, 53 KB

english, 2009

33

Diverse Heterocyclic Scaffolds as Allosteric Inhibitors of AKT

Kettle, Jason G., Brown, Simon, Crafter, Claire, Davies, Barry R., Dudley, Phillippa, Fairley, Gary, Faulder, Paul, Fillery, Shaun, Greenwood, Hannah, Hawkins, Janet

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 1.70 MB

english, 2012

34

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

Kettle, Jason G., Ward, Richard A., Griffen, Ed

Journal:

Year:

2010

Language:

english

File:

PDF, 176 KB

english, 2010

35

Toward the Comprehensive Systematic Enumeration and Synthesis of Novel Kinase Inhibitors Based on a 4-Anilinoquinazoline Binding Mode

Kettle, Jason G., Ward, Richard A.

Journal:

Journal of Chemical Information and Modeling

Year:

2010

Language:

english

File:

PDF, 301 KB

english, 2010

36

Discovery of 4-Amino- N -[(1 S )-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7 H -pyrrolo[2,3- d ]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases

Addie, Matt, Ballard, Peter, Buttar, David, Crafter, Claire, Currie, Gordon, Davies, Barry R., Debreczeni, Judit, Dry, Hannah, Dudley, Philippa, Greenwood, Ryan, Johnson, Paul D., Kettle, Jason G., La

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 920 KB

english, 2013

37

Expanding medicinal chemistry space

Barker, Andy, Kettle, Jason G., Nowak, Thorsten, Pease, J. Elizabeth

Journal:

Drug Discovery Today

Year:

2013

Language:

english

File:

PDF, 304 KB

english, 2013

38

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

Barlaam, Bernard, Anderton, Judith, Ballard, Peter, Bradbury, Robert H., Hennequin, Laurent F. A., Hickinson, D. Mark, Kettle, Jason G., Kirk, George, Klinowska, Teresa, Lambert-van der Brempt, Christ

Journal:

ACS Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 2.13 MB

english, 2013

39

Highly regioselective Buchwald–Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries

Burton, Rebecca J., Crowther, Mandy L., Fazakerley, Neal J., Fillery, Shaun M., Hayter, Barry M., Kettle, Jason G., McMillan, Caroline A., Perkins, Paula, Robins, Peter, Smith, Peter M., Williams, Emm

Journal:

Tetrahedron Letters

Year:

2013

Language:

english

File:

PDF, 293 KB

english, 2013

40

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

Goldberg, Frederick W., Kettle, Jason G., Xiong, Jian, Lin, Daoguang

Journal:

Year:

2014

Language:

english

File:

PDF, 526 KB

english, 2014

41

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

Goldberg, Frederick W., Kettle, Jason G., Kogej, Thierry, Perry, Matthew W.D., Tomkinson, Nick P.

Journal:

Drug Discovery Today

Year:

2015

Language:

english

File:

PDF, 1012 KB

english, 2015

42

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

Ashford, Anne L., Oxley, David, Kettle, Jason, Hudson, Kevin, Guichard, Sylvie, Cook, Simon J., Lochhead, Pamela A.

Journal:

Biochemical Journal

Year:

2014

Language:

english

File:

PDF, 1.12 MB

english, 2014

43

Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation

Winter, Jon J. G., Anderson, Malcolm, Blades, Kevin, Brassington, Claire, Breeze, Alexander L., Chresta, Christine, Embrey, Kevin, Fairley, Gary, Faulder, Paul, Finlay, M. Raymond V., Kettle, Jason G.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 9.61 MB

english, 2015

44

Discovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors To Explore a MEK Resistance Hypothesis

Kettle, Jason G., Ballard, Peter, Bardelle, Catherine, Cockerill, Mark, Colclough, Nicola, Critchlow, Susan E., Debreczeni, Judit, Fairley, Gary, Fillery, Shaun, Graham, Mark A., Goodwin, Louise, Guic

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.67 MB

english, 2015

45

A γ-lactamase from cereal infecting Fusarium spp. catalyses the first step in the degradation of the benzoxazolinone class of phytoalexins

Kettle, Andrew J., Carere, Jason, Batley, Jacqueline, Benfield, Aurelie H., Manners, John M., Kazan, Kemal, Gardiner, Donald M.

Journal:

Fungal Genetics and Biology

Year:

2015

Language:

english

File:

PDF, 1.62 MB

english, 2015

46

The Fdb3 transcription factor of the Fusarium Detoxification of Benzoxazolinone gene cluster is required for MBOA but not BOA degradation in Fusarium pseudograminearum

Kettle, Andrew J., Carere, Jason, Batley, Jacqueline, Manners, John M., Kazan, Kemal, Gardiner, Donald M.

Journal:

Fungal Genetics and Biology

Year:

2016

Language:

english

File:

PDF, 1.65 MB

english, 2016

47

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

Kettle, Jason G., Alwan, Husam, Bista, Michal, Breed, Jason, Davies, Nichola L., Eckersley, Kay, Fillery, Shaun, Foote, Kevin M., Goodwin, Louise, Jones, David R., Käck, Helena, Lau, Alan, Nissink, J.

Journal:

Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 3.49 MB

english, 2016

48

Synthesis of 1,2,3,4,5,7-Hexahydro-6H-azocino[4,3-b]indol-6-ones as Intermediates for the Synthesis of Apparicine

A. Joule, John, Roberts, David, G. Kettle, Jason

Journal:

Year:

2010

File:

PDF, 1.35 MB

2010

49

Synthesis of 1,2,3,4,5,7-Hexahydro-6H-azocino[4,3-b]indol-6-ones as Intermediates for the Synthesis of Apparicine

A. Joule, John, Roberts, David, G. Kettle, Jason

Journal:

Year:

2010

Language:

english

File:

PDF, 1.35 MB

english, 2010

50

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

Kettle, Jason G., Wilson, David M.

Journal:

Drug Discovery Today

Year:

2016

Language:

english

File:

PDF, 1.42 MB

english, 2016