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Browsing publications by Dr Ian Hardcastle.

Newcastle AuthorsTitleYearFull text
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 profile2024
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 index2024
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 interactions2022
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
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
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
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 generation2019
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 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 Notification2018
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 approach2018
Amy Heptinstall
Dr Celine Cano
Dr Ian Hardcastle
Recent advances in CDK inhibitors for cancer therapy2018
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-Arylaminopurines2017
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 Ian Hardcastle
Protein-protein interaction inhibitors2017
Dr Ian Hardcastle
Protein-Protein Interaction Inhibitors in Cancer2017
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
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
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
Tristan Reuillon
Duncan Miller
Stephanie Myers
Dr Lauren Molyneux
Dr Celine Cano
et al.
Pyrrolcarboxamide Derivatives for the Inhibition of ERK52016
Dr Ian Hardcastle
Aryne generation vs. Truce-Smiles and fries rearrangements during the Kobayashi fragmentation reaction: a new bi-aryl synthesis2015
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
Bian Zhang
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Small-molecule MDM2-p53 inhibitors: recent advances2015
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
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
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 Ian Hardcastle
Resistance acquisition to MDM2 inhibitors2014
Dr Ian Hardcastle
Targeting the MDM2-p53 protein-protein interaction: Design, discovery, and development of novel anticancer agents2014
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
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 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 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
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
Professor Martin Noble
Dr Ian Hardcastle
Professor Jane Endicott
Understanding small-molecule binding to MDM2: Insights into structural effects of isoindolinone inhibitors from NMR spectroscopy2011
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
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 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
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
Dr Ian Hardcastle
Inhibitors of the MDM2-p53 interaction as anticancer drugs2007
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
Professor William Clegg
et al.
Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase2007
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 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
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
Dr Ian Hardcastle
Dr Amir Mirza
An evaluation of the ability of pifithrin-alpha and -beta to inhibit p53 function in two wild-type p53 human tumor cell lines2005
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
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
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
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
Kerry Louise Sayle
Dr Veronique Mesguiche
Rachel Parsons
Professor Jane Endicott
Professor Martin Noble
et al.
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 22002
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
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 Ian Hardcastle
Pentafluoronitrobenzene a novel scaffold for the solid-phase synthesis of 2,4,6-substituted-3,5-difluoronitrobenzene libraries2002
Dr Ian Hardcastle
Pifithrin alpha and beta do not inhibit ionising radiation dependent p53 responses in human wild type p53 ovarian and colon cell lines2002
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
Dr Ian Hardcastle
Synthesis of 6,8-substituted-5,7-difluoro-3,4-dihydro-1H-quinoxalin-2-ones via reductive cyclisation of 2,4,6-substituted-3,5-difluoronitrobenzenes2002
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
Dr Ian Hardcastle
Meg Barber
Polymer-assisted solution-phase library synthesis of 4-alkoxy-2-hydroxy-3,5,6-trifluorobenzoic acids2001
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
Dr Ian Hardcastle
Synthesis of the farnesyl ether 2,3,5-trifluoro-6-hydroxy-4-[(E,E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yloxy] nitrobenzene, and related compounds containing a substituted hydroxytrifluorophenyl residue: Novel inhibitors of protein farnesyltransferase, geranylgeranyltransferase I and squalene synthase2000
Dr Ian Hardcastle
Idoxifene antagonises estradiol-dependent MCF-7 breast cancer xenograft grown through sustained induction of apoptosis1999
Dr Ian Hardcastle
Inhibition of protein prenylation by metabolites of limonene1999
Dr Ian Hardcastle
Solid-phase synthesis of novel inhibitors of Farnesyl Transferase1999
Dr Ian Hardcastle
Length increase of the side chain of idoxifene does not improve its antagonistic potency in breast-cancer cell lines1998
Dr Ian Hardcastle
Synthesis and DNA reactivity of alpha-hydroxylated metabolites of nonsteroidal antiestrogens1998
Dr Ian Hardcastle
Tamoxifen induces selective membrane association of protein kinase C epsilon in MCF-7 human breast cancer cells1998
Dr Ian Hardcastle
A convenient, large scale synthesis of abiraterone acetate [3-acetoxy-17-(3-pyridyl)androsta-5,16-diene], a potential new drug for the treatment of prostate cancer1997
Dr Ian Hardcastle
Minor products of reaction of DNA with alpha-acetoxytamoxifen1997
Dr Ian Hardcastle
Antiestrogens as calmodulin antagonists1996
Dr Ian Hardcastle
Homologues of idoxifene: variation of estrogen receptor binding and calmodulin antagonism with chain length1996