Publications by Professor Roger Griffin - ePrints

Browsing publications by Professor Roger Griffin.

Newcastle Authors	Title	Year
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 Inhibitor	2022
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 Interaction	2021
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 kinase	2020
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 BRD4	2019
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 Chemotherapy	2019
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 ACTIVITY	2017
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	2017
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 2017055860	2017
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 inhibition	2017
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 radiation	2016
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 kinase	2016
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 cancer	2016
Dr Victorovich Zaytsev James Pickles Dr Suzannah Harnor Dr Alistair Henderson Mohammed Al Yasiri et al.	Concise syntheses of bridged morpholines	2016
Tristan Reuillon Dr Sari Alhasan Dr Gary Beale Annalisa Bertoli Alfie Brennan et al.	Design and synthesis of biphenyl and biphenyl ether inhibitors of sulfatases	2016
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) inhibitors	2016
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 study	2016
Tristan Reuillon Duncan Miller Stephanie Myers Dr Lauren Molyneux Dr Celine Cano et al.	Pyrrolcarboxamide Derivatives for the Inhibition of ERK5	2016
Elisa Meschini Dr Regina Mora Vidal Dr Mathew Martin Dr Will Stanley Tristan Reuillon et al.	Identification and characterization of an irreversible inhibitor of CDK2	2015
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 sulfatases	2015
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 Approach	2015
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 SKP2	2015
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 Mode	2014
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 isoindolinones	2014
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 inhibitors	2014
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 complex	2014
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 therapy	2014
Dr Mathew Martin Elisa Meschini Lan Wang Dr Regina Mora Vidal Tristan Reuillon et al.	Identification and characterization of an irreversible inhibitor of CDK2	2014
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 heterocycles	2014
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 levels	2014
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]FLT	2014
Dr Benoit Carbain Christopher Coxon Honorine Lebraud Dr Kris Elliott Christopher Matheson et al.	Trifluoroacetic Acid in 2,2,2-Trifluoroethanol Facilitates S_NAr Reactions of Heterocycles with Arylamines	2014
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 interaction	2014
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 Activity	2013
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 interactions	2013
Sarah Cully Dr Celine Cano Emeritus Professor Bernard Golding Professor Roger Griffin Professor John Lunec et al.	Regiospecific synthesis of isoindolinones as MDM2 inhibitors	2013
Dr Celine Cano Professor Roger Griffin	The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design	2013
Honorine Lebraud Dr Celine Cano Dr Benoit Carbain Dr Ian Hardcastle Dr Ross Harrington et al.	Trifluoroethanol solvent facilitates selective N-7 methylation of purines	2013
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 Nek2	2012
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 cancer	2012
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-3K	2012
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 response	2012
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 groups	2012
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 agents	2012
Professor Roger Griffin	Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family	2012
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 derivatives	2012
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 domain	2011
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 Potency	2011
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 isoindolinones	2011
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 Glycoprotein	2011
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 NU6301	2011
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 Closure	2011
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 inhibitors	2010
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 Chemotype	2010
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 inhibitors	2010
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 inhibitors	2010
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 inhibitors	2010
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 S_N2 reactivity of 2,2,2-trifluoroethoxysulfonates	2010
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 cytotoxicity	2009
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 NU6301	2008
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 Interaction	2008
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 leukemia	2008
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 lines	2008
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 interaction	2008
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 therapy	2007
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 acids	2007
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 kinase	2007
Dr Olivier Barbeau Dr Celine Cano Professor Roger Griffin Dr Ian Hardcastle Professor William Clegg et al.	Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase	2007
Dr Francesco Marchetti Kerry Louise Sayle Dr Johanne Bentley Professor William Clegg Professor Nicola Curtin et al.	Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6- aminopyrimidine inhibitors of cyclin-dependent kinase 2	2007
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 inhibitors	2006
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 NU7441	2006
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 elimination	2006
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 scaffold	2006
Professor Roger Griffin	Clinical potential of DNA repair inhibitors	2005
Dr Olivier Barbeau Emeritus Professor Bernard Golding Professor Roger Griffin Dr Ian Hardcastle	Design and synthesis of novel DNA-dependent protein kinase (DNA-PK) inhibitors	2005
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) inhibitors	2005
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 approach	2005
Professor Herbie Newell Professor Roger Griffin Richard Davison Lan Wang Professor Nicola Curtin et al.	Effect of cell cycle inhibition on cisplatin-induced cytotoxicity	2005
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 kinase	2005
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 scaffold	2005
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 interaction	2005
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 interaction	2005
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 elimination	2005
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-regulation	2005
Emeritus Professor Bernard Golding Dr Ian Hardcastle Professor Roger Griffin	Searching for potent CDK inhibitors using a new variant of the Cope elimination	2005
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 elimination	2005
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 vitro	2005
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) polymerase	2004
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 libraries	2004
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 2	2004
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 inhibitors	2004
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 glycoprotein	2004
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 2	2003
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 trifluoroethanol	2003
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 2	2003
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 inhibitors	2003
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 kinase	2002
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 inhibitors	2002
Professor Roger Griffin	Combinatorial methods for identifying antitumour kinase inhibitors	2002
Dr Julian Scott Northen Professor William 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]pyrimidines	2002
Dr Ian Hardcastle Emeritus Professor Bernard Golding Professor Roger Griffin	Designing inhibitors of cyclin-dependent kinases	2002
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 inhibitors	2002
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 structure	2002
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 derivatives	2002
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 inhibitor	2002
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 activity	2001
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 compounds	2001
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 design	2001
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 vitro	2001
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 design	2001
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 cdk2	2001
Martin Stockley Professor William 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 NU3121	2000
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) polymerase	2000
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 inhibitors	2000
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 profiles	2000
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 profiles	2000
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) guanine	2000
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) polymerase	2000
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 inhibitors	2000
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) inhibitors	1999
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 binding	1999
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) polymerase	1999
Emeritus Professor Bernard Golding Professor William Clegg Dr Mark Elsegood Professor Roger Griffin	Protecting-group strategies for the synthesis of N4-substituted, and N1,N8-disubstituted spermidines, exemplified by hirudonine	1999
Professor William Clegg Dr Mark Elsegood Professor Roger Griffin Emeritus Professor Bernard Golding	Synthesis of 3-alkoxy- and 3-alkylamino-2-alkyl-3-arylisoindolinones	1999
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 lines	1998
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 studies	1998
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 kinases	1998
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 NU1064	1998
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 agents	1997
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)polymerase	1996
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-Therapy	1995
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 hirudonine	1994
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