Dr Celine Cano Professor Jane Endicott Dr Ian Hardcastle Dr Claire Jennings Suzanne Kyle et al. | Discovery of ASTX295, a potent, next-generation small molecule antagonist of MDM2 with differentiated pharmacokinetic profile | 2024 |
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Dr Elaine Willmore Suzanne Kyle Dr Yan Zhao Huw Thomas Dr Kenneth Rankin et al. | Targeting the MDM2-p53 interaction: Time- and concentration-dependent studies in tumor and normal human bone marrow cells reveal strategies for an enhanced therapeutic index | 2024 |
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Nikol Zografou Barredo Dr Alex Hallatt Dr Jennyfer Goujon-Ricci Dr Celine Cano
| A beginner’s guide to current synthetic linker strategies towards VHL-recruiting PROTACs | 2023 |
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Duncan Miller Dr Suzannah Harnor Dr Mathew Martin Dr Richard Noble Professor Steve Wedge et al. | Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy | 2023 |
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Dr Suzannah Harnor Dr Celine Cano
| Advanced approaches of developing targeted covalent drugs | 2022 |
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Gemma Davison Dr Mathew Martin Dr Shannon Turberville Selma Dormen Dr Richard Heath et al. | Mapping ligand interactions of bromodomains BRD4 and ATAD2 with FragLites and PepLites ─ Halogenated probes of druglike and peptide-like molecular interactions | 2022 |
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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 |
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Islam Al-Khawaldeh Dr Christine Basmadjian Dr Cinzia Bordoni Dr Suzannah Harnor Amy Heptinstall et al. | An alkynylpyrimidine-based covalent inhibitor that targets a unique cysteine in NF-κB-inducing kinase (NIK) | 2021 |
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Edwige Picazo Amy Heptinstall Dr Celine Cano Emeritus Professor Bernard Golding Professor Mike Waring et al. | Cyclisations and fragmentations in the alkylation of 6-chloro-5-hydroxy-4-aminopyrimidines with aminoalkyl chlorides | 2021 |
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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 |
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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 |
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Dr Brian Ford Dr Shruti Chachra Ahmed Alshawi Alfie Brennan Dr Suzannah Harnor et al. | Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge | 2020 |
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Dr Celine Cano
| Molecular dynamics simulations reveal the determinants of cyclin-dependent kinase 2 inhibition by 5-nitrosopyrimidine derivatives | 2020 |
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Dr Christine Basmadjian Dr Celine Cano
| Nek7 conformational flexibility and inhibitor binding probed through protein engineering of the R-spine | 2020 |
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Dr Adam Potts Dr Celine Cano Professor Simon Thomas Dr Simon Hill
| Synthetic cannabinoid receptor agonists: classification and nomenclature | 2020 |
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Daniel Wood Daniel Lopez Fernandez Leanne Knight Islam Al-Khawaldeh Dr Conghao Gai et al. | FragLites - minimal, halogenated fragments displaying pharmacophore doublets. An efficient approach to druggability assessment and hit generation | 2019 |
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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 |
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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 |
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Dr Simon Hill Dr Michael Dunn Dr Celine Cano Dr Suzannah Harnor Dr Ian Hardcastle et al. | Human Toxicity Caused by Indole and Indazole Carboxylate Synthetic Cannabinoid Receptor Agonists: From Horizon Scanning to Notification | 2018 |
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Duncan Miller Dr Mathew Martin Santosh Adhikari Alfie Brennan Professor Jane Endicott et al. | Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach | 2018 |
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Amy Heptinstall Dr Celine Cano Dr Ian Hardcastle
| Recent advances in CDK inhibitors for cancer therapy | 2018 |
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Dr Celine Cano Dr Suzannah Harnor Dr Elaine Willmore Professor Steve Wedge
| Targeting DNA-PK as a Therapeutic Approach in Oncology | 2018 |
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Judith Unterlass Dr Arnaud Basle Dr Julie Tucker Dr Celine Cano Professor Martin Noble et al. | Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer | 2018 |
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Christopher Coxon Dr Suzannah Harnor Dr Mathew Martin Dr Benoit Carbain Emeritus Professor Bernard Golding et al. | Cyclin-Dependent Kinase (CDK) Inhibitors; Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines | 2017 |
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Dr Suzannah Harnor Alfie Brennan Dr Celine Cano
| Inhibition of the DNA-Dependent Protein Kinase for Cancer Therapy | 2017 |
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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 |
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Dr Suzannah Harnor James Pickles Dr Celine Cano
| Modulation of the DNA-Damage Response by Inhibitors of the Phosphatidylinositol 3-Kinase Related Kinase (PIKK) Family | 2017 |
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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 |
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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 |
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Judith Unterlass Dr Arnaud Basle Dr Julie Tucker Dr Celine Cano Professor Martin Noble et al. | Structural insights into the enzymatic activity and potential substrate promiscuity of human 3-phosphoglycerate dehydrogenase (PHGDH) | 2017 |
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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 |
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Dr Suzannah Harnor Alfie Brennan Dr Celine Cano
| Targeting DNA-Dependent Protein Kinase for Cancer Therapy | 2017 |
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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 |
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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 |
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Dr Victorovich Zaytsev James Pickles Dr Suzannah Harnor Dr Alistair Henderson Mohammed Al Yasiri et al. | Concise syntheses of bridged morpholines | 2016 |
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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 |
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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 |
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Tristan Reuillon Duncan Miller Stephanie Myers Dr Lauren Molyneux Dr Celine Cano et al. | Pyrrolcarboxamide Derivatives for the Inhibition of ERK5 | 2016 |
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Emeritus Professor Bernard Golding Dr Celine Cano
| Synthesis and Biological Evaluation of N2-Substituted 2,4-Diamino-6-cyclohexylmethoxy-5-nitrosopyrimidines and Related 5-Cyano-NNO-azoxy Derivatives as Cyclin-Dependent Kinase 2 (CDK2) Inhibitors | 2016 |
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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 |
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Judith Unterlass Nabila Aljufri Sophie Bex Dr Celine Cano Professor Martin Noble et al. | Towards structure-based drug design of 3-phosphoglycerate dehydrogenase inhibitors | 2015 |
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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 |
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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 |
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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 |
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Emily Mould Philip Berry Dr David Jamieson Dr Chris Hill Dr Celine Cano et al. | Identification of dual DNA-PK MDR1 inhibitors for the potentiation of cytotoxic drug activity | 2014 |
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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 |
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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 |
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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 |
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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 Arylamines | 2014 |
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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 |
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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 |
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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 |
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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 |
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Dr Celine Cano Professor Roger Griffin
| The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design | 2013 |
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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 |
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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 |
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Dr Michele Tavecchio Dr Joanne Martin Dr Celine Cano Professor Herbie Newell Professor Nicola Curtin et al. | Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination | 2012 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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Dr Celine Cano
| Five-membered rings with two adjacent heteroatoms with at least one other element | 2008 |
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Dr Celine Cano
| Five-membered rings with two non-adjacent heteroatoms with at least one other element | 2008 |
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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 |
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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 |
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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 |
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Dr Celine Cano
| A bis(η5-cyclopentadienyl)cobalt complex of a bis-dithiolene: a chemical analogue of the metal centres of the DMSO reductase family of molybdenum and tungsten enzymes, in particular ferredoxin aldehyde oxidoreductase | 2005 |
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Dr Celine Cano
| Regio- and Enantioselective Synthesis of Novel Functionalized Pyranopyrrolidines by 1,3-Dipolar Cycloaddition of Carbohydrates | 2005 |
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Dr Celine Cano
| Stereoselective Cycloaddition on Carbohydrates for the Synthesis of New Bicyclic Oxazolidines Bearing a Quaternary Bridgehead | 2005 |
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