Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Roger John Griffin"'
Autor:
Roger John Griffin, Martin E.M. Noble, James M. McDonnell, Anna Watson, Jane A. Endicott, Stuart J. Kemp, Bernard T. Golding, Lynette A. Smyth, Christiane Riedinger, Eric Valeur, Ian R. Hardcastle
Publikováno v:
Journal of the American Chemical Society. 130:16038-16044
In this study we present a method for defining the binding modes of a set of structurally related isoindolinone inhibitors of the MDM2-p53 interaction. This approach derives the location and orientation of isoindolinone binding, based on an analysis
Autor:
Robert Almassy, Theodore J. Boritzki, Karen A. Maegley, Bernard T. Golding, Suzanne Kyle, Huw D. Thomas, Stephen E. Webber, Tikhe Jayashree Girish, A. Hilary Calvert, Nicola J. Curtin, Xiao-Hong Yu, Jianke Li, Zdenek Hostomsky, Roger John Griffin, David Richard Newell, Anne Ekkers, Cathy Zhang, Robert Arnold Kumpf, Christopher R. Calabrese, Lan-Zhen Wang
Publikováno v:
Journal of Medicinal Chemistry. 47:5467-5481
The design, synthesis, and biological evaluation of potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) are reported. A novel series of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones were designed using a combination of protein structure
Autor:
Yi Chen, Lan-Zhen Wang, J Bentley, AE Gibson, Philip J. Jewsbury, Bernard T. Golding, D.J. Pratt, FT Boyle, H.J. Whitfield, Mesguiche, Martin E.M. Noble, J Menyerol, Jane A. Endicott, Ian R. Hardcastle, Roger John Griffin, David Richard Newell, C.E. Arris, Nicola J. Curtin
Publikováno v:
Journal of Medicinal Chemistry. 47:3710-3722
The adenosine 5'-triphosphate (ATP) competitive cyclin-dependent kinase inhibitor O(6)-cyclohexylmethylguanine (NU2058, 1) has been employed as the lead in a structure-based drug discovery program resulting in the discovery of the potent CDK1 and -2
Autor:
Bernard T. Golding, Laurent Rigoreau, Graeme Cameron Murray Smith, Jonathan James Hollick, Niall M. B. Martin, Ian R. Hardcastle, Roger John Griffin, Caroline Richardson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3083-3086
6-aryl-2-morpholin-4-yl-4H-pyran-4-ones and 6-aryl-2-morpholin-4-yl-4H-thiopyran-4-ones were synthesised and evaluated as potential inhibitors of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). Several compounds in each series exhibited
Autor:
Huw D. Thomas, Anne Ekker, Stephen E. Webber, Christopher R. Calabrese, Nicola J. Curtin, Robert Almassy, Karen A. Maegley, Rena N. Mansour, Lan-Zhen Wang, Robert Arnold Kumpf, A. Hilary Calvert, Cathy Zhang, Scott E. Zook, Jianke Li, Bernard T. Golding, Tikhe Jayashree Girish, Xiao-Hong Yu, Suzanne Kyle, Zdenek Hostomsky, Theodore J. Boritzki, Thoresen Lars Henrik, David Richard Newell, Kanyin E. Zhang, Stacie S. Canan Koch, Roger John Griffin
Publikováno v:
Journal of Medicinal Chemistry. 45:4961-4974
A series of novel compounds have been designed that are potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1), and the activity and physical properties have been characterized. The new structural classes, 3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]
Autor:
Nicola J. Curtin, Bernard T. Golding, Philip J. Jewsbury, E.A Sausville, David Richard Newell, Alison M. Lawrie, AE Gibson, A.H Calvert, W. Yu, Roger John Griffin, R Schultz, FT Boyle, CE Arris, Louise N. Johnson, S Grant, Elspeth F. Garman, Martin E.M. Noble, Jane A. Endicott
Publikováno v:
Journal of Medicinal Chemistry. 43:2797-2804
Substituted guanines and pyrimidines were tested as inhibitors of cyclin B1/CDK1 and cyclin A3/CDK2 and soaked into crystals of monomeric CDK2. O6-Cyclohexylmethylguanine (NU2058) was a competitive inhibitor of CDK1 and CDK2 with respect to ATP (Ki v
Autor:
Pete Smith, A. Hilary Calvert, HC Barlow, Roger John Griffin, Karen J. Bowman, Bernard T. Golding, David Richard Newell, Nicola J. Curtin, Peter J. Loughlin, B Huang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:585-589
The synthesis and biological evaluation of potent 4,8-dibenzylaminopyrimidopyrimidine nucleoside transport inhibitors, with reduced binding to α1-acid glycoprotein, is reported.
Autor:
Bernard T. Golding, Mark R. J. Elsegood, William Clegg, Andrew Mitchinson, Roger John Griffin
Publikováno v:
Scopus-Elsevier
Methods are described for the preparation of derivatives of the polyamines 1,4-diaminobutane (putrescine) and N-(3-aminopropyl)-1,4-diaminobutane (spermidine) in which a particular amino group is modified with, e.g., a guanidino function. Specific am
Autor:
Bernard T. Golding, Roger John Griffin, Annalisa Bertoli, Tristan Reuillon, Miller Duncan Charles
Publikováno v:
ChemInform. 44
The protection-deprotection strategy comprises reaction of phenols (I) with sulfonylbis(methylimidazole) (II) to provide aryl imidazole sulfonates (III), which are activated by reaction with trimethyloxonium tetrafluoroborate, before further reaction
Autor:
Daniel L. Rathbone, Simon B Bedford, Roger John Griffin, Malcolm F. G. Stevens, Charmaine Paulina Quarterman, John A. Slack
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:157-160
Water-soluble phosphate and glycine carbamate prodrugs of the cytotoxic agent Combretastatin A4 (1) have been prepared. The phosphate prodrug was degraded slowly in plasma at 37°C. The degradation was accelerated by the addition of alkaline phosphat