259 results on '"Hardcastle, Ian R."'
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2. Tamoxifen induces selective membrane association of protein kinase C epsilon in MCF‐7 human breast cancer cells
3. Mapping Ligand Interactions of Bromodomains BRD4 and ATAD2 with FragLites and PepLites─Halogenated Probes of Druglike and Peptide-like Molecular Interactions
4. Parallel Optimisation of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Chemical Tool
5. An alkynylpyrimidine-based covalent inhibitor that targets a unique cysteine in NF-κB-inducing kinase (NIK)
6. Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein–Protein Interaction by a Scaffold-Hopping Approach
7. Targeting the MDM2–p53 Protein–Protein Interaction
8. Contributors
9. Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction
10. Understanding Small-Molecule Binding to MDM2: Insights into Structural Effects of Isoindolinone Inhibitors from NMR Spectroscopy
11. 2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase
12. Length increase of the side chain of idoxifene does not improve its antagonistic potency in breast-cancer cell lines
13. FragLites—Minimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation
14. Recent advances in CDK inhibitors for cancer therapy
15. Human Toxicity Caused by Indole and Indazole Carboxylate Synthetic Cannabinoid Receptor Agonists: From Horizon Scanning to Notification
16. Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach
17. Solid-phase synthesis of novel inhibitors of Farnesyl Transferase
18. Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2–p53 and MDMX–p53 protein–protein interactions† †Electronic supplementary information (ESI) available: Experimental details for compound synthesis, analytical data for all compounds and intermediates. Details for the biological evaluation. Further details for the modeling. Table of combustion analysis data. See DOI: 10.1039/c3md00161jClick here for additional data file
19. Referee report. For: Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade [version 1; referees: 2 approved]
20. Analysis of chemical shift changes reveals the binding modes of isoindolinone inhibitors of the MDM2-p53 interaction
21. Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines
22. 2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinaseElectronic supplementary information (ESI) available: Kinase profiling, assay details, synthetic procedures and characterisation data for all compounds; including aniline precursors. All cell lines were supplied by the American Type Culture Collection, Manassas, Virginia, United States. All animal experiments performed were conducted under a UK Government Home Office License in accordance with relevant national laws. All procedures were reviewed and approved by the Newcastle University Animal Welfare Ethical Board and performed according to institutional guidelines. See DOI: 10.1039/d0md00074d
23. FragLitesMinimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation.
24. Chapter 13 - Targeting the MDM2–p53 Protein–Protein Interaction: Design, Discovery, and Development of Novel Anticancer Agents
25. Structure-guided design of purine-based probes for selective Nek2 inhibition
26. Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo antitumour activity in colorectal cancer
27. High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors
28. TP53 mutant MDM2-amplified cell lines selected for resistance to MDM2-p53 binding antagonists retain sensitivity to ionizing radiation
29. Small-Molecule MDM2-p53 Inhibitors: Recent Advances
30. Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach
31. MDM2-p53 protein–protein interaction inhibitors: A-ring substituted isoindolinones
32. DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain
33. Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors
34. Abstract 5451: Profiling inhibitors of MDM2:p53 and MDMX:p53 in relation to MDMX protein levels
35. Trifluoroacetic Acid in 2,2,2-Trifluoroethanol Facilitates SNAr Reactions of Heterocycles with Arylamines
36. Model system for irreversible inhibition of Nek2: thiol addition to ethynylpurines and related substituted heterocycles
37. 8-Substituted O6-Cyclohexylmethylguanine CDK2 Inhibitors: Using Structure-Based Inhibitor Design to Optimize an Alternative Binding Mode
38. 1-Substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones Endowed with Dual DNA-PK/PI3-K Inhibitory Activity
39. ChemInform Abstract: Trifluoroethanol Solvent Facilitates Selective N-7 Methylation of Purines.
40. Trifluoroethanol solvent facilitates selective N-7 methylation of purines
41. 8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK)
42. Characterisation of a Tip60 Specific Inhibitor, NU9056, in Prostate Cancer
43. Abstract 919: Design and preclinical pharmacological evaluation of a cleavable succinate ester solubilizing group for isoindolinone MDM2-p53 protein-protein interaction inhibitors
44. Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives
45. Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301
46. Isoindolinone Inhibitors of the Murine Double Minute 2 (MDM2)-p53 Protein−Protein Interaction: Structure−Activity Studies Leading to Improved Potency
47. Versatile synthesis of functionalised dibenzothiophenes via Suzuki coupling and microwave-assisted ring closure
48. 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
49. ChemInform Abstract: Polymer-Assisted Solution-Phase Library Synthesis of 4-Alkoxy-2-hydroxy-3,5,6-trifluorobenzoic Acids.
50. Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitors
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