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Ian Hardcastle

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Chemicals & Drugs

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Honorine Lebraud; Celine Cano; Benoit Carbain; Roger J Griffin; Ian R Hardcastle; Ross W Harrington; Bernard T Golding
Trifluoroethanol solvent facilitates selective N-7 methylation of purines.
Kate M Clapham; Faye Craven; Bernard T Golding; Roger J Griffin; Karen Haggerty; Ian R Hardcastle; Gavin Jones; Tommy Rennison; Pia Thommes; Attilla Ting; Julia Bárdos; Céline Cano
Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives.
Anna F Watson; Qing Xu; Yan Zhao; Karim Bennaceur; Catherine J Drummond; Jane A Endicott; Bernard T Golding; Roger J Griffin; Karen Haggerty; Junfeng Liu; Xiaohong Lu; John Lunec; James M McDonnell; David R Newell; Martin E M Noble; Charlotte H Revill; Christiane Riedinger; Ian R Hardcastle
MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.

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All Publications

2013: Honorine Lebraud; Celine Cano; Benoit Carbain; Roger J Griffin; Ian R Hardcastle; Ross W Harrington; Bernard T Golding
Trifluoroethanol solvent facilitates selective N-7 methylation of purines.
Organic & biomolecular chemistry 2013;11(11):1874-8.
2012: Kate M Clapham; Faye Craven; Bernard T Golding; Roger J Griffin; Karen Haggerty; Ian R Hardcastle; Gavin Jones; Tommy Rennison; Pia Thommes; Attilla Ting; Julia Bárdos; Céline Cano
Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives.
Organic & biomolecular chemistry 2012;10(33):6747-57.
2011: Anna F Watson; Qing Xu; Yan Zhao; Karim Bennaceur; Catherine J Drummond; Jane A Endicott; Bernard T Golding; Roger J Griffin; Karen Haggerty; Junfeng Liu; Xiaohong Lu; John Lunec; James M McDonnell; David R Newell; Martin E M Noble; Charlotte H Revill; Christiane Riedinger; Ian R Hardcastle
MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
Bioorganic & medicinal chemistry letters 2011;21(19):5916-9.
2011: Sonsoles Rodriguez-Aristegui; Lauren Barrett; Céline Cano; Kate M Clapham; Marine Desage-El Murr; Roger J Griffin; Ian R Hardcastle; Sara L Payne; Tommy Rennison; Caroline Richardson; Bernard T Golding
Versatile synthesis of functionalised dibenzothiophenes via Suzuki coupling and microwave-assisted ring closure.
Organic & biomolecular chemistry 2011;9(17):6066-74.
2010: Sara L Payne; Sonsoles Rodriguez-Aristegui; Julia Bárdos; Céline Cano; Bernard T Golding; Ian R Hardcastle; Marcus Peacock; Nahida Parveen; Roger J Griffin
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(12):3649-53.
2010: Christopher Wong; Roger J Griffin; Ian R Hardcastle; Julian S Northen; Lan Z Wang; Bernard T Golding
Synthesis of sulfonamide-based kinase inhibitors from sulfonates by exploiting the abrogated SN2 reactivity of 2,2,2-trifluoroethoxysulfonates.
Organic & biomolecular chemistry 2010;8(10):2457-64.
2010: Francesco Marchetti; Céline Cano; Nicola J Curtin; Bernard T Golding; Roger J Griffin; Karen Haggerty; David R Newell; Rachel J Parsons; Sara L Payne; Lan Z Wang; Ian R Hardcastle
Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitors.
Organic & biomolecular chemistry 2010;8(10):2397-407.
2010: Céline Cano; Bernard T Golding; Karen Haggerty; Ian R Hardcastle; Marcus Peacock; Roger J Griffin
Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK).
Organic & biomolecular chemistry 2010;8(8):1922-8.
2008: Marine Desage-El Murr; Celine Cano; Bernard T Golding; Ian R Hardcastle; Marc Hummersome; Mark Frigerio; Nicola J Curtin; Keith A Menear; Caroline Richardson; Graeme C M Smith; Roger J Griffin
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).
Bioorganic & medicinal chemistry letters 2008;18(17):4885-90.
2007: Olivier R Barbeau; Celine Cano-Soumillac; Roger J Griffin; Ian R Hardcastle; Graeme C M Smith; Caroline Richardson; William Clegg; Ross W Harrington; Bernard T Golding
Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase.
Organic & biomolecular chemistry 2007;5(16):2670-7.
2007: Francesco Marchetti; Kerry L Sayle; Johanne Bentley; William Clegg; Nicola J Curtin; Jane A Endicott; Bernard T Golding; Roger J Griffin; Karen Haggerty; Ross W Harrington; Veronique Mesguiche; David R Newell; Martin E M Noble; Rachel J Parsons; David J Pratt; Lan Z Wang; Ian R Hardcastle
Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2.
Organic & biomolecular chemistry 2007;5(10):1577-85.
2007: Jonathan J Hollick; Laurent Rigoreau; Celine Cano-Soumillac; Xiaoling Cockcroft; Nicola J Curtin; Mark Frigerio; Bernard T Golding; Sophie Guiard; Ian R Hardcastle; Ian Hickson; Marc G Hummersone; Keith A Menear; Niall M B Martin; Ian Matthews; David R Newell; Rachel Ord; Caroline J Richardson; Graeme C M Smith; Roger J Griffin
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.
Journal of medicinal chemistry 2007;50(8):1958-72.
2007: Sonja Seeberger; Roger J Griffin; Ian R Hardcastle; Bernard T Golding
A new strategy for the synthesis of taurine derivatives using the 'safety-catch' principle for the protection of sulfonic acids.
Organic & biomolecular chemistry 2007;5(1):132-8.
2006: Sonsoles Rodriguez Aristegui; Marine Desage El-Murr; Bernard T Golding; Roger J Griffin; Ian R 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.
Organic letters 2006;8(26):5927-9.
2006: Ian R Hardcastle; Shafiq U Ahmed; Helen Atkins; Gillian Farnie; Bernard T Golding; Roger J Griffin; Sabrina Guyenne; Claire Hutton; Per Kallblad; Stuart J Kemp; Martin S Kitching; David R Newell; Stefano Norbedo; Julian S Northen; Rebecca J Reid; K Saravanan; Henriëtte M G Willems; John Lunec
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.
Journal of medicinal chemistry 2006;49(21):6209-21.
2006: Roger J Griffin; Andrew Henderson; Nicola J Curtin; Aude Echalier; Jane A Endicott; Ian R Hardcastle; David R Newell; Martin E M Noble; Lan Z Wang; Bernard T Golding
Searching for cyclin-dependent kinase inhibitors using a new variant of the cope elimination.
Journal of the American Chemical Society 2006;128(18):6012-3.
2005: Ian R Hardcastle; Xiaoling Cockcroft; Nicola J Curtin; Marine Desage El-Murr; Justin J J Leahy; Martin Stockley; Bernard T Golding; Laurent Rigoreau; Caroline Richardson; Graeme C M Smith; Roger J Griffin
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.
Journal of medicinal chemistry 2005;48(24):7829-46.
2005: Marzia Pennati; Allyson J Campbell; Maria Curto; Mara Binda; Yuzhu Cheng; Lan Z Wang; Nicola J Curtin; Bernard T Golding; Roger J Griffin; Ian R Hardcastle; Andrew Henderson; Nadia Zaffaroni; David R Newell
Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation.
Molecular cancer therapeutics 2005;4(9):1328-37.
2005: Ian R Hardcastle; Shafiq U Ahmed; Helen Atkins; A Hilary Calvert; Nicola J Curtin; Gillian Farnie; Bernard T Golding; Roger J Griffin; Sabrina Guyenne; Claire Hutton; Per Kallblad; Stuart J Kemp; Martin S Kitching; David R Newell; Stefano Norbedo; Julian S Northen; Rebecca J Reid; K Saravanan; Henriëtte M G Willems; John Lunec
Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction.
Bioorganic & medicinal chemistry letters 2005;15(5):1515-20.
2005: Roger J Griffin; Gabriele Fontana; Bernard T Golding; Sophie Guiard; Ian R Hardcastle; Justin J J Leahy; Niall Martin; Caroline Richardson; Laurent Rigoreau; Martin Stockley; Graeme C M Smith
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.
Journal of medicinal chemistry 2005;48(2):569-85.
2004: Justin J J Leahy; Bernard T Golding; Roger J Griffin; Ian R Hardcastle; Caroline Richardson; Laurent Rigoreau; Graeme C M Smith
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
Bioorganic & medicinal chemistry letters 2004;14(24):6083-7.
2004: Ian R Hardcastle; Christine E Arris; Johanne Bentley; F Thomas Boyle; Yuzhu Chen; Nicola J Curtin; Jane A Endicott; Ashleigh E Gibson; Bernard T Golding; Roger J Griffin; Philip Jewsbury; Jerome Menyerol; Veronique Mesguiche; David R Newell; Martin E M Noble; David J Pratt; Lan Z Wang; Hayley J Whitfield
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.
Journal of medicinal chemistry 2004;47(15):3710-22.
2003: Hayley J Whitfield; Roger J Griffin; Ian R Hardcastle; Andrew Henderson; Jerome Meneyrol; Veronique Mesguiche; Kerry L Sayle; Bernard T Golding
Facilitation of addition-elimination reactions in pyrimidines and purines using trifluoroacetic acid in trifluoroethanol.
Chemical communications (Cambridge, England) 2003;(22):2802-3.
2003: Jonathan J Hollick; Bernard T Golding; Ian R Hardcastle; Niall Martin; Caroline Richardson; Laurent Rigoreau; Graeme C M Smith; Roger J Griffin
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).
Bioorganic & medicinal chemistry letters 2003;13(18):3083-6.
2003: Kerry L Sayle; Johanne Bentley; F Thomas Boyle; A Hilary Calvert; Yuzhu Cheng; Nicola J Curtin; Jane A Endicott; Bernard T Golding; Ian R Hardcastle; Philip Jewsbury; Veronique Mesguiche; David R Newell; Martin E M Noble; Rachel J Parsons; David J Pratt; Lan Z Wang; Roger J Griffin
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.
Bioorganic & medicinal chemistry letters 2003;13(18):3079-82.
2003: Veronique Mesguiche; Rachel J Parsons; Christine E Arris; Johanne Bentley; F Thomas Boyle; Nicola J Curtin; Thomas G Davies; Jane A Endicott; Ashleigh E Gibson; Bernard T Golding; Roger J Griffin; Philip Jewsbury; Louise N Johnson; David R Newell; Martin E M Noble; Lan Z Wang; Ian R Hardcastle
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.
Bioorganic & medicinal chemistry letters 2003;13(2):217-22.
2002: Thomas G Davies; Johanne Bentley; Christine E Arris; F Thomas Boyle; Nicola J Curtin; Jane A Endicott; Ashleigh E Gibson; Bernard T Golding; Roger J Griffin; Ian R Hardcastle; Philip Jewsbury; Louise N Johnson; Veronique Mesguiche; David R Newell; Martin E M Noble; Julie A Tucker; Lan Wang; Hayley J Whitfield
Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor.
Nature structural biology 2002;9(10):745-9.
2002: Ian R Hardcastle; Bernard T Golding; Roger J Griffin
Designing inhibitors of cyclin-dependent kinases.
Annual review of pharmacology and toxicology 2002;42():325-48.