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Browsing publications by Professor Roger Griffin.

Newcastle AuthorsTitleYearFull text
Duncan Miller
Tristan Reuillon
Dr Lauren Molyneux
Dr Tim Blackburn
Dr Noel Edwards
et al.
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor2022
Dr Ian Hardcastle
Dr Ruth Bawn
Dr Tim Blackburn
Dr Celine Cano
Dr Sarah Cully
et al.
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction2021
Christopher Matheson
Christopher Coxon
Dr Benoit Carbain
Dr Ian Hardcastle
Dr Suzannah Harnor
et al.
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase2020
Stephanie Myers
Duncan Miller
Dr Lauren Molyneux
Dr Mercedeh Arasta
Dr Ruth Bawn
et al.
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD42019
Dr Catherine Willoughby
Huw Thomas
Dr Elaine Willmore
Suzanne Kyle
Dr Anita Wittner
et al.
Selective DNA-PKcs Inhibition Extends the Therapeutic Index of Localized Radiotherapy and Chemotherapy2019
Professor David Rees
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
Duncan Miller
et al.
ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION HAVING ANTICANCER ACTIVITY2017
Professor David Rees
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
Duncan Miller
et al.
Preparation of isoindolinones as inhibitors of the MDM2-​p53 interaction having anticancer activity2017
Professor David Rees
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
Duncan Miller
et al.
Preparation of isoindolinones as inhibitors of the MDM2-​p53 interaction having anticancer activity;WO 20170558602017
Dr Christopher Wong
Dr Ian Hardcastle
Christopher Matheson
Professor Herbie Newell
Dr Mangaleswaran Sivaprakasam
et al.
Structure-guided design of purine-based probes for selective Nek2 inhibition2017
Dr Catherine Drummond
Arman Esfandiari
Dr Xiaohong Lu
Dr Claire Hutton
Dr Jennifer Jackson
et al.
TP53 mutant MDM2-amplified cell lines selected for resistance to MDM2-p53 binding antagonists retain sensitivity to ionizing radiation2016
Christopher Coxon
Dr Celine Cano
Emeritus Professor Bernard Golding
Professor Roger Griffin
A new tool for the chemical genetic investigation of the Plasmodium falciparum Pfnek-2 NIMA-related kinase2016
Dr Gary Beale
Dr Emma Haagensen
Huw Thomas
Lan Wang
Charlotte Revill
et al.
Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo anti-tumour activity in colorectal cancer2016
Dr Victorovich Zaytsev
James Pickles
Dr Suzannah Harnor
Dr Alistair Henderson
Mohammed Al Yasiri
et al.
Concise syntheses of bridged morpholines2016
Tristan Reuillon
Dr Sari Alhasan
Dr Gary Beale
Annalisa Bertoli
Alfie Brennan
et al.
Design and synthesis of biphenyl and biphenyl ether inhibitors of sulfatases2016
Stephanie Myers
Dr Ruth Bawn
Betty Cottyn
Dr Lauren Molyneux
Dr Celine Cano
et al.
High-throughput screening and hit validation of extracellular-related kinase 5 (ERK5) inhibitors2016
Professor Roger Griffin
Emeritus Professor Bernard Golding
New derivatives of the antimalarial drug Pyrimethamine in the control of melanoma tumor growth: an in vitro and in vivo study2016
Tristan Reuillon
Duncan Miller
Stephanie Myers
Dr Lauren Molyneux
Dr Celine Cano
et al.
Pyrrolcarboxamide Derivatives for the Inhibition of ERK52016
Elisa Meschini
Dr Regina Mora Vidal
Dr Mathew Martin
Dr Will Stanley
Tristan Reuillon
et al.
Identification and characterization of an irreversible inhibitor of CDK22015
Duncan Miller
Dr Benoit Carbain
Dr Gary Beale
Dr Sari Alhasan
Professor Helen Reeves
et al.
Regioselective sulfamoylation at low temperature enables concise syntheses of putative small molecule inhibitors of sulfatases2015
Dr Andrey Zaytsev
Dr Barry Dodd
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Xiaohong Lu
et al.
Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach2015
Andrew Shouksmith
Laura Evans
Professor Deborah Tweddle
Duncan Miller
Dr Elaine Willmore
et al.
Synthesis and Activity of Putative Small-​Molecule Inhibitors of the F-​Box Protein SKP22015
Dr Benoit Carbain
Dr Allyson Campbell
Dr Celine Cano
Professor Jane Endicott
Emeritus Professor Bernard Golding
et al.
8-Substituted O-6-Cyclohexylmethylguanine CDK2 Inhibitors: Using Structure-Based Inhibitor Design to Optimize an Alternative Binding Mode2014
Alex Liu
Dr Catherine Drummond
Professor Jane Endicott
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
An X-ray crystal structure-based understanding of the inhibition of the MDM2-p53 protein-protein interaction by isoindolinones2014
Honorine Lebraud
Emeritus Professor Bernard Golding
Elisa Meschini
Dr Celine Cano
Lan Wang
et al.
Anticancer agents targeted against cyclin-dependent kinase 2 (CDK2): Structure-based design of irreversible and reversible inhibitors2014
Andrew Shouksmith
Laura Evans
Professor Roger Griffin
Emeritus Professor Bernard Golding
Professor Herbie Newell
et al.
Design and synthesis of putative small-molecule inhibitors targeting the SCFSKP2 E3 ligase complex2014
Dr Ruth Bawn
Tristan Reuillon
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Ian Hardcastle
et al.
Development of extracellular signal-regulated kinase 5 (ERK5) inhibitors for anti-cancer therapy2014
Dr Mathew Martin
Elisa Meschini
Lan Wang
Dr Regina Mora Vidal
Tristan Reuillon
et al.
Identification and characterization of an irreversible inhibitor of CDK22014
Honorine Lebraud
Christopher Coxon
Vicky Archard
Carlo Bawn
Dr Benoit Carbain
et al.
Model system for irreversible inhibition of Nek2: thiol addition to ethynylpurines and related substituted heterocycles2014
Dr Susan Tudhope
Dr Yan Zhao
Dr Anita Wittner
Annalisa Bertoli
Santosh Adhikari
et al.
Profiling inhibitors of MDM2: p53 and MDMX: p53 in relation to MDMX protein levels2014
Dr Suzannah Harnor
Dr Tommy Rennison
Dr Martin Galler
Dr Celine Cano
Professor Roger Griffin
et al.
Synthesis of 3 '-deoxy-3'-fluorothymidine (FLT) 5 '-O-glucuronide: a reference standard for imaging studies with [18F]FLT2014
Dr Benoit Carbain
Christopher Coxon
Honorine Lebraud
Dr Kris Elliott
Christopher Matheson
et al.
Trifluoroacetic Acid in 2,2,2-Trifluoroethanol Facilitates SNAr Reactions of Heterocycles with Arylamines2014
Annalisa Bertoli
Santosh Adhikari
Dr Suzannah Harnor
Dr Yan Zhao
Professor John Lunec
et al.
Validation studies with small-molecule modulators of the MDM2/MDMX-p53 binding interaction2014
Dr Celine Cano
Dr Kappusamy Saravanan
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
1-Substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones Endowed with Dual DNA-PK PI3-K Inhibitory Activity2013
Dr Tommy Rennison
Sonsoles Rodriguez-Aristegui
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
Development of potent inhibitors of DNA-dependent protein kinase (DNA-PK)2013
Dr Tim Blackburn
Christopher Coxon
Dr Xiaohong Lu
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2-p53 and MDMX-p53 protein-protein interactions2013
Sarah Cully
Dr Celine Cano
Emeritus Professor Bernard Golding
Professor Roger Griffin
Professor John Lunec
et al.
Regiospecific synthesis of isoindolinones as MDM2 inhibitors2013
Dr Celine Cano
Professor Roger Griffin
The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design2013
Honorine Lebraud
Dr Celine Cano
Dr Benoit Carbain
Dr Ian Hardcastle
Dr Ross Harrington
et al.
Trifluoroethanol solvent facilitates selective N-7 methylation of purines2013
Dr Benoit Carbain
Christopher Coxon
Honorine Lebraud
Christopher Matheson
David Turner
et al.
2-arylamino-6-ethynylpurines as Potent Irreversible Inhibitors of the Mitotic Kinase Nek22012
Dr Kelly Coffey
Dr Tim Blackburn
Susan Cook
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer2012
Dr Joanne Martin
Michael Batey
Dr Yan Zhao
Dr Celine Cano
Dr Michele Tavecchio
et al.
Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K2012
Professor Roger Griffin
Differential effects of the glycolysis inhibitor 2-deoxy-D-glucose on the activity of pro-apoptotic agents in metastatic melanoma cells, and induction of a cytoprotective autophagic response2012
Tristan Reuillon
Annalisa Bertoli
Professor Roger Griffin
Duncan Miller
Emeritus Professor Bernard Golding
et al.
Efficacious N-protection of O-aryl sulfamates with 2,4-dimethoxybenzyl groups2012
Emeritus Professor Bernard Golding
Professor Roger Griffin
Mechanism-based design, synthesis and biological studies of N-5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents2012
Professor Roger Griffin
Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family2012
Dr Tommy Rennison
Faye Craven
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Karen Haggerty
et al.
Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives2012
Dr Kate Smith
Emeritus Professor Bernard Golding
Elizabeth Griffin
Professor Roger Griffin
Dr Ian Hardcastle
et al.
DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain2011
Dr Ian Hardcastle
Alex Liu
Dr Eric Valeur
Anna Watson
Shafiq Ahmed
et al.
Isoindolinone Inhibitors of the Murine Double Minute 2 (MDM2)-p53 Protein-Protein Interaction: Structure-Activity Studies Leading to Improved Potency2011
Dr Karim Bennaceur
Dr Catherine Drummond
Professor Jane Endicott
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
MDM2-p53 protein-protein interaction inhibitors: A-ring substituted isoindolinones2011
Dr Kappusamy Saravanan
Hannah Barlow
Marion Barton
Professor Hilary Calvert
Emeritus Professor Bernard Golding
et al.
Nucleoside Transport Inhibitors: Structure-Activity Relationships for Pyrimido[5,4-d]pyrimidine Derivatives That Potentiate Pemetrexed Cytotoxicity in the Presence of α1-Acid Glycoprotein2011
Huw Thomas
Dr Celine Roche
Dr Johanne Bentley
Dr Ian Hardcastle
Emeritus Professor Bernard Golding
et al.
Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU63012011
Sonsoles Rodriguez-Aristegui
Dr Lauren Molyneux
Dr Celine Cano
Dr Marine Desage-El-Murr
Professor Roger Griffin
et al.
Versatile Synthesis of Functionalised Dibenzothiophenes via Suzuki Coupling and Microwave-assisted Ring Closure2011
Dr Celine Cano
Emeritus Professor Bernard Golding
Dr Karen Haggerty
Dr Ian Hardcastle
Professor Roger Griffin
et al.
Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK)2010
Elisa Meschini
Professor Jane Endicott
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Professor Herbie Newell
et al.
Design and synthesis of dual CDK2 and CDK7 inhibitors2010
Dr Kate Smith
Dr Tommy Rennison
Sonsoles Rodriguez-Aristegui
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Development of potent inhibitors of DNA-dependent protein kinase (DNA-PK)2010
Dr Celine Cano
Dr Olivier Barbeau
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
DNA-Dependent Protein Kinase (DNA-PK) Inhibitors. Synthesis and Biological Activity of Quinolin-4-one and Pyridopyrimidin-4-one Surrogates for the Chromen-4-one Chemotype2010
Sara Payne
Sonsoles Rodriguez-Aristegui
Dr Celine Cano
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors2010
Dr Benoit Carbain
Dr Celine Roche
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
et al.
Structure-based design of C8-substituted O6-alkylguanine CDK1 and 2 inhibitors2010
Dr Francesco Marchetti
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitors2010
Dr Christopher Wong
Professor Roger Griffin
Dr Ian Hardcastle
Dr Julian Scott Northen
Lan Wang
et al.
Synthesis of sulfonamide-based kinase inhibitors from sulfonates by exploiting the abrogated SN2 reactivity of 2,2,2-trifluoroethoxysulfonates2010
Huw Thomas
Dr Kappusamy Saravanan
Lan Wang
Mei Lin
Dr Julian Scott Northen
et al.
Preclinical evaluation of a novel pyrimidopyrimidine for the prevention of nucleoside and nucleobase reversal of antifolate cytotoxicity2009
Professor Herbie Newell
Huw Thomas
Lan Wang
Dr Celine Roche
Dr Ian Hardcastle
et al.
[abstract] Preclinical in vitro and in vivo evaluation of the cyclin dependent kinase 2 inhibitor NU6102 and a water pro-drug NU63012008
Dr Celine Cano
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Professor Nicola Curtin
Professor Roger Griffin
et al.
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK)2008
Professor Jane Endicott
Stuart Kemp
Dr Lucy Smyth
Dr Eric Valeur
Emeritus Professor Bernard Golding
et al.
Analysis of Chemical Shift Changes Reveals the Binding Modes of Isoindolinone Inhibitors of the MDM2-p53 Interaction2008
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Karen Haggerty
Dr Ian Hardcastle
et al.
Development of Potent Water-soluble Inhibitors of DNA-Dependent Protein Kinase (DNA-PK)2008
Dr Elaine Willmore
Dr sarah Johnson
Dr Tryfonia Mainou-Fowler
Professor Graham Jackson
Dr Celine Cano
et al.
DNA-dependent protein kinase is a therapeutic target and an indicator of poor prognosis in B-cell chronic lymphocytic leukemia2008
Dr Kappusamy Saravanan
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Karen Haggerty
et al.
Identification of potent water-soluble DNA-dependent protein kinase (DNA-PK) inhibitors using a small-molecule library approach [abstract]2008
Dr Xiaomei Lu
Alex Liu
Dr Ian Hardcastle
Professor Roger Griffin
Emeritus Professor Bernard Golding
et al.
MDM2 and MDMX status as a determinant of in vitro cellular sensitivity to MDM2 antagonists in human tumour cell lines2008
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Claire Hutton
Professor John Lunec
Professor Herbie Newell
et al.
MEDI 147-Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction2008
Michael Batey
Dr Laurent Rigoreau
Professor Roger Griffin
Professor Herbie Newell
Professor Nicola Curtin
et al.
Potent in vitro and in vivo radiosensitisation by the selective DNA-dependent protein kinase inhibitor KU-0060648 [abstract]2008
Professor Roger Griffin
[Meeting Abstract] DNA damage-activated kinases as targets for cancer therapy2007
Sonja Seeberger
Professor Roger Griffin
Dr Ian Hardcastle
Emeritus Professor Bernard Golding
A new strategy for the synthesis of taurine derivatives using the 'safety-catch' principle for the protection of sulfonic acids2007
Jonathan Hollick
Dr Laurent Rigoreau
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase2007
Dr Olivier Barbeau
Dr Celine Cano
Professor Roger Griffin
Dr Ian Hardcastle
Emeritus Professor Bill Clegg
et al.
Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase2007
Dr Francesco Marchetti
Kerry Louise Sayle
Dr Johanne Bentley
Emeritus Professor Bill Clegg
Professor Nicola Curtin
et al.
Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6- aminopyrimidine inhibitors of cyclin-dependent kinase 22007
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Ian Hardcastle
Judicious application of allyl protecting groups for the synthesis of 2-morpholin-4-yl-4-oxo-4H-chromen-8-yl triflate, a key precursor of DNA-dependent protein kinase inhibitors2006
Dr Yan Zhao
Huw Thomas
Michael Batey
Dr Ian Cowell
Professor Roger Griffin
et al.
Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU74412006
Professor Roger Griffin
Andrew Henderson
Professor Nicola Curtin
Professor Jane Endicott
Dr Ian Hardcastle
et al.
Searching for cyclin-dependent kinase inhibitors using a new variant of the cope elimination2006
Dr Ian Hardcastle
Dr Shafiq Ahmed
Helen Atkins
Gillian Farnie
Emeritus Professor Bernard Golding
et al.
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold2006
Professor Roger Griffin
Clinical potential of DNA repair inhibitors2005
Dr Olivier Barbeau
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Ian Hardcastle
Design and synthesis of novel DNA-dependent protein kinase (DNA-PK) inhibitors2005
Professor Roger Griffin
Dr Olivier Barbeau
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Design and synthesis of novel pyridopyrimidin-4-one and quinolin-4-one DNA-dependent protein kinase (DNA-PK) inhibitors2005
Dr Ian Hardcastle
Professor Nicola Curtin
Justin John James Leahy
Martin Stockley
Emeritus Professor Bernard Golding
et al.
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach2005
Professor Herbie Newell
Professor Roger Griffin
Richard Davison
Lan Wang
Professor Nicola Curtin
et al.
Effect of cell cycle inhibition on cisplatin-induced cytotoxicity2005
Dr Olivier Barbeau
Professor Roger Griffin
Dr Ian Hardcastle
Emeritus Professor Bernard Golding
Efficient synthesis of 8-substituted 2-morpholine-4-yl-quinolin-4-ones: Potent inhibitors of DNA-dependent protein kinase2005
Dr Ian Hardcastle
Shafiq Ahmed
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Claire Hutton
et al.
Inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold2005
Stuart Kemp
Dr Ian Hardcastle
Dr Shafiq Ahmed
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
Isoindolinone based inhibitors of the MDM2-p53 protein-protein interaction2005
Dr Ian Hardcastle
Dr Shafiq Ahmed
Professor Alan Calvert
Professor Nicola Curtin
Gillian Farnie
et al.
Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction2005
Professor Roger Griffin
Dr YuZhu Cheng
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
Potent CDK2 inhibitors generated using a variant of the cope elimination2005
Dr Allyson Campbell
Dr YuZhu Cheng
Lan Wang
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: A possible role for survivin down-regulation2005
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Professor Roger Griffin
Searching for potent CDK inhibitors using a new variant of the Cope elimination2005
Andrew Henderson
Dr YuZhu Cheng
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
Searching for potent CDK2 inhibitors using a variant of the Cope elimination2005
Professor Roger Griffin
Emeritus Professor Bernard Golding
Sophie Guiard
Dr Ian Hardcastle
Justin John James Leahy
et al.
Selective benzopyranone and pyrimido[2,1-alpha]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: Synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro2005
Dr Christopher Calabrese
Professor Nicola Curtin
Suzanne Kyle
Huw Thomas
Lan Wang
et al.
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1- hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase2004
Justin John James Leahy
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Ian Hardcastle
Dr Laurent Rigoreau
et al.
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries2004
Dr Ian Hardcastle
Dr Christine Arris
Dr Johanne Bentley
Professor Nicola Curtin
Professor Jane Endicott
et al.
N2-substituted O6-cyclohexylmethylguanine derivatives: Potent inhibitors of cyclin-dependent kinases 1 and 22004
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Suzanne Kyle
Professor Roger Griffin
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors2004
Professor Nicola Curtin
Hannah Barlow
Professor Alan Calvert
Richard Davison
Emeritus Professor Bernard Golding
et al.
Resistance-modifying agents. 11. Pyrimido[5,4-d]pyrimidine modulators of antitumor drug activity. Synthesis and structure-activity relationships for nucleoside transport inhibition and binding to α1-acid glycoprotein2004
Jonathan Hollick
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Laurent Rigoreau
Professor Roger Griffin
et al.
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-dependent protein kinase (DNA-PK)2003
Dr Veronique Mesguiche
Rachel Parsons
Dr Christine Arris
Dr Johanne Bentley
Professor Nicola Curtin
et al.
4-Alkoxy-2,6-diaminopyrimidine derivatives: Inhibitors of cyclin dependent kinases 1 and 22003
Hayley Whitfield
Professor Roger Griffin
Dr Ian Hardcastle
Dr Alistair Henderson
Dr Jerome Meneyrol
et al.
Facilitation of addition-elimination reactions in pyrimidines and purines using trifluoroacetic acid in trifluoroethanol2003
Kerry Louise Sayle
Dr Johanne Bentley
Professor Alan Calvert
Dr YuZhu Cheng
Professor Nicola Curtin
et al.
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 22003
Professor Nicola Curtin
Professor Herbie Newell
Professor Alan Calvert
Professor Roger Griffin
Emeritus Professor Bernard Golding
et al.
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors2003
Jonathan Hollick
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Ian Hardcastle
Justin John James Leahy
et al.
Application of combinatorial chemistry for the identification of pyran-4-one and thiopyran-4-one inhibitors of DNA-dependent protein kinase2002
Professor Roger Griffin
Dr Ian Hardcastle
Dr Laurent Rigoreau
Martin Stockley
Justin John James Leahy
et al.
Cassette dosing iv and ip of novel DNA dependent protein kinase inhibitors2002
Professor Roger Griffin
Combinatorial methods for identifying antitumour kinase inhibitors2002
Dr Julian Scott Northen
Emeritus Professor Bill Clegg
Professor Nicola Curtin
Professor Roger Griffin
Emeritus Professor Bernard Golding
et al.
Controlled stepwise conversion of 2,4,6,8-tetrachloropyrimido-[5,4-d ]pyrimidine into 2,4,6,8-tetrasubstituted pyrimido[5,4-d]pyrimidines2002
Dr Ian Hardcastle
Emeritus Professor Bernard Golding
Professor Roger Griffin
Designing inhibitors of cyclin-dependent kinases2002
Professor Roger Griffin
Dr Ian Hardcastle
Dr Laurent Rigoreau
Martin Stockley
Justin John James Leahy
et al.
High throughput pharmacokinetics of novel DNA-dependent protein kinase inhibitors2002
Dr Christopher Calabrese
Professor Nicola Curtin
Suzanne Kyle
Huw Thomas
Lan Wang
et al.
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis, and X-ray cocrystal structure2002
Dr Ashleigh Gibson
Dr Christine Arris
Dr Johanne Bentley
Professor Nicola Curtin
Professor Jane Endicott
et al.
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O6-substituted guanine derivatives2002
Dr Johanne Bentley
Dr Christine Arris
Professor Nicola Curtin
Professor Jane Endicott
Dr Ashleigh Gibson
et al.
Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor2002
Professor Nicola Curtin
Dr Stephen Barton
Michael Batey
Dr Christopher Calabrese
Professor Alan Calvert
et al.
Anti-cancer chemosensitization in vitro and in vivo by a novel potent poly(ADP-ribose) polymerase (PARP1) inhibitor, TBI-361.2001
Peter Smith
Huw Thomas
Hannah Barlow
Professor Roger Griffin
Emeritus Professor Bernard Golding
et al.
In vitro and in vivo properties of novel nucleoside transport inhibitors with improved pharmacological properties that potentiate antifolate activity2001
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Ian Hardcastle
et al.
Inhibiting the MDM2-p53 interaction using low molecular weight compounds2001
Professor Roger Griffin
Investigations on the biological properties of the lipophilic DHFR-inhibitory benzoprims reveal non-folate modes of action and opportunities for anti-cancer drug design2001
Dr Stephany Veuger
Professor barbara Durkacz
Emeritus Professor Bernard Golding
Professor Roger Griffin
Professor Herbie Newell
et al.
Radiosensitization by novel inhibitors of PARP, PI, and DNA-PK, NU7026, in vitro2001
Professor Martin Noble
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Dr Ashleigh Gibson
et al.
Structural and thermodynamic validation of inactive cdk2 as a template for structure-based drug design2001
Professor Martin Noble
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Structure based design of a potent inhibitor of cdk22001
Martin Stockley
Emeritus Professor Bill Clegg
Emeritus Professor Bernard Golding
Nicola Martin
Dr Laurent Rigoreau
et al.
Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035)2001
Peter Smith
Huw Thomas
Hannah Barlow
Professor Roger Griffin
Emeritus Professor Bernard Golding
et al.
In vitro activity and in vivo pharmacology of two novel nucleoside transport inhibitors, NU3108 and NU31212000
Professor Nicola Curtin
Professor Alan Calvert
Professor barbara Durkacz
Professor Roger Griffin
Emeritus Professor Bernard Golding
et al.
Chemopotentiation studies with two classes of potent (polyADP-ribose) polymerase (PARP) inhibitors in human lung and colon carcinoma cell lines.2000
Dr Christopher Calabrese
Professor Nicola Curtin
Michael Batey
Huw Thomas
Suzanne Kyle
et al.
Design and evaluation of novel potent inhibitors of poly (ADP-ribose) polymerase2000
Professor Roger Griffin
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Dr Ashleigh Gibson
et al.
Design, synthesis, and biological evaluation of O-6-alkylguanine and O-4-alkylpyrimidine cyclin-dependent kinase inhibitors2000
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Professor Jane Endicott
Emeritus Professor Bernard Golding
et al.
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles2000
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Dr Ashleigh Gibson
Emeritus Professor Bernard Golding
et al.
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles2000
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
O6-substituted guanines and 4-substituted pyrimidines: a novel class of antiproliferative cyclin dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.2000
Professor Roger Griffin
Dr Christine Arris
Dr Christine Bleasdale
Professor Alan Calvert
Professor Nicola Curtin
et al.
Resistance-modifying agents. 8. Inhibition of O6-alkylguanine-DNA alkyltransferase by O6-alkenyl-, O6-cycloalkenyl-, and O6-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O6-(1-cyclopentenylmethyl) guanine2000
Alex White
Professor Alan Calvert
Professor Nicola Curtin
Professor Roger Griffin
Professor Herbie Newell
et al.
Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase2000
Hannah Barlow
Professor Nicola Curtin
Professor Alan Calvert
Emeritus Professor Bernard Golding
Professor Herbie Newell
et al.
Resistance-modifying agents. Part 7: 2,6-Disubstituted-4,8-dibenzylaminopyrimido[5,4-d]pyrimidines that inhibit nucleoside transport in the presence of α1-acid glycoprotein (AGP)2000
Dr Johanne Bentley
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Professor Jane Endicott
et al.
Structure-activity relationships and cellular effects of novel purine- and pyrimidine-based cyclin dependent kinase inhibitors2000
Professor Roger Griffin
Hannah Barlow
Professor Nicola Curtin
Professor Alan Calvert
Emeritus Professor Bernard Golding
et al.
2,6-Disubstituted-4,8-dibenzylaminopyrimido[5,4-d]pyrimidines as nucleoside transport inhibitors: Structure-activity relationships for binding to alpha(1)-acid glycoprotein (AGP)1999
Professor Herbie Newell
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Dr Ashleigh Gibson
et al.
Antiproliferative cyclin dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.1999
Dr Christine Arris
Professor Alan Calvert
Professor Nicola Curtin
Dr Ashleigh Gibson
Emeritus Professor Bernard Golding
et al.
In vitro growth activity of novel purine- and pyrimidine-based CDK1 and CDK2 inhibitors.1999
Peter Smith
Hannah Barlow
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Novel dipyridamole analogues potentiate the in vitro activity of MTA (LY231514) in the presence of alpha(1)-acid glycoprotein.1999
Professor Nicola Curtin
Suzanne Kyle
Lan Wang
Professor barbara Durkacz
Professor Roger Griffin
et al.
Potentiation of temozolomide and topotecan growth inhibition by novel potent benzimidazole poly(ADP-ribose) polymerase (PARP) inhibitors1999
Professor Nicola Curtin
Professor Alan Calvert
Emeritus Professor Bernard Golding
Professor Roger Griffin
Professor Herbie Newell
et al.
Potentiation of the cytotoxicity of thymidylate synthase (TS) inhibitors by dipyridamole analogues with reduced α1-acid glycoprotein binding1999
Dr Christopher Calabrese
Huw Thomas
Michael Batey
Professor Nicola Curtin
Professor Roger Griffin
et al.
Preclinical pharmacology of novel substituted benzimidazoles - potent inhibitors of poly (ADP-ribose) polymerase1999
Emeritus Professor Bernard Golding
Emeritus Professor Bill Clegg
Dr Mark Elsegood
Professor Roger Griffin
Protecting-group strategies for the synthesis of N4-substituted, and N1,N8-disubstituted spermidines, exemplified by hirudonine1999
Emeritus Professor Bill Clegg
Dr Mark Elsegood
Professor Roger Griffin
Emeritus Professor Bernard Golding
Synthesis of 3-alkoxy- and 3-alkylamino-2-alkyl-3-arylisoindolinones1999
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Professor Roger Griffin
Professor Herbie Newell
et al.
2-phenylbenzimidazole-4-carboxamides are potent inhibitors of the DNA repair enzyme poly(ADP-ribose)-polymerase (PARP)1998
Professor Craig Robson
Professor Roger Griffin
Chemical synthesis and biological properties of novel fluorescent antifolates in Pgp- and MRP-overexpressing tumour cell lines1998
Professor Jane Endicott
Professor Martin Noble
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Insights into CDK inhibitor design from X-ray crystallographic studies1998
Professor Alan Calvert
Professor Nicola Curtin
Professor Jane Endicott
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
O-6-alkylguanines as selective inhibitors of cyclin dependent kinases1998
Alex White
Emeritus Professor Bernard Golding
Professor Roger Griffin
Professor Nicola Curtin
Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU10641998
Professor Roger Griffin
Professor Alan Calvert
Professor Nicola Curtin
Professor Herbie Newell
Emeritus Professor Bernard Golding
et al.
Resistance-modifying agents. 5.1 Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP)1998
Professor Craig Robson
Professor Roger Griffin
Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: Activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents1997
Dr Christine Arris
Dr Christine Bleasdale
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Mechanism-based inhibition of O-6-methylguanine-DNA methyltransferase.1996
Professor Roger Griffin
Alex White
Kenneth Bowman
Professor Alan Calvert
Professor Nicola Curtin
et al.
Novel benzimidazole and quinazolinone inhibitors of the DNA repair enzyme Poly(ADP-ribose)polymerase1996
Professor Roger Griffin
Professor Nicola Curtin
Professor Herbie Newell
Emeritus Professor Bernard Golding
Professor barbara Durkacz
et al.
The Role of Inhibitors of Poly(Adp-Ribose) Polymerase as Resistance-Modifying Agents in Cancer-Therapy1995
Emeritus Professor Bernard Golding
Professor Roger Griffin
Discrimination of spermidine amino functions by a new protecting group strategy; application to the synthesis of guanidinylated polyamines, including hirudonine1994
Dr Christine Arris
Dr Christine Bleasdale
Professor Alan Calvert
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Probing the active site and mechanism of action of O-6-methylguanine-DNA methyltransferase with substrate-analogs to (O-6-substituted guanines)1994