Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Michael John Johnston"'
Autor:
Philip Alan Skone, Iain Uings, Davina Humphreys, Diane M. Coe, George Hardy, Simon J. F. Macdonald, Doug J. Minick, Richard Loiseau, Haydn Terence Jones, Iain M. McLay, David House, Derek A. Demaine, Michael John Johnston, Graham G. A. Inglis, Margaret Clackers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4737-4745
Starting from an established series of non-steroidal glucocorticoid receptor (GR) agonists, a large array was designed where a metabolically labile benzoxazinone moiety was replaced. Initial hits bound to GR but lacked agonist activity. Following two
Autor:
Melanie Washington, Davina Humphreys, Lesley Nisbet, Philip Alan Skone, Royston C. B. Copley, Simon J. F. Macdonald, Graham G. A. Inglis, Richard J. Upton, Mike D. Barker, Margaret Clackers, Victoria Vinader, Haydn Terence Jones, Michael John Johnston, Iain M. McLay, Derek A. Demaine, Stephen E. Shanahan, David House, Richard Loiseau, Dan Tape, Michael V. Haase, Francois Pacquet, Iain Uings
Publikováno v:
Journal of Medicinal Chemistry. 49:4216-4231
The tetrahydronaphthalene-benzoxazine glucocorticoid receptor (GR) partial agonist 4b was optimized to produce potent full agonists of GR. Aromatic ring substitution of the tetrahydronaphthalene leads to weak GR antagonists. Discovery of an "agonist
Autor:
Graham G. A. Inglis, George Hardy, Philip Alan Skone, Simon J. F. Macdonald, Gemma Veitch, Diane M. Coe, Haydn Terence Jones, Iain M. McLay, Margaret Clackers, Derek A. Demaine, Richard Loiseau, Gordon G. Weingarten, Iain Uings, Keith Biggadike, Michael John Johnston, Deborah Needham, Mohamed Boudjelal, David House, Davina Humphreys
Publikováno v:
Journal of medicinal chemistry. 50(26)
The synthesis and biological activity of tetrahydronaphthalene derivatives coupled to various heterocycles are described. These compounds are potent glucocorticoid receptor agonists with efficacy selectivity in an NFkappaB glucocorticoid receptor (GR
Autor:
Simon J. F. Macdonald, Michael John Johnston, Mike D. Barker, Amanda Morris, Jonathon Hacon, Stephen E. Shanahan, Graham G. A. Inglis
Publikováno v:
ChemInform. 38
Reactions and purifications, including carbon-carbon bond forming reactions, can be carried out on a cellulose support on which the substrates are non-covalently absorbed.
Autor:
Victoria Vinader, Davina Humphreys, Philip Alan Skone, Iain M. McLay, John Martin Pritchard, Derek A. Demaine, Michael John Johnston, Stephen E. Shanahan, Haydn Terence Jones, Mark Salter, Francois Pacquet, Iain Uings, Simon J. F. Macdonald, Mike D. Barker, Margaret Clackers
Publikováno v:
Journal of medicinal chemistry. 48(14)
Structurally related glucocorticoid receptor (GR) binders were docked into the GR active site to select the binding mode closest to the true docking mode. This process, termed an “agreement docking method”, led to the design of tetrahydronaphthal