Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Jon Graham Anthony Steadman"'
Autor:
Andrew Charlton, Stephen J. Medhurst, Laura J. Chambers, Livermore David, Brian Peter Slingsby, Andy Billinton, Lee William Page, Anton D. Michel, Daryl S. Walter, Jon Graham Anthony Steadman, Shilina Roman, Sadhana Patel, Elena Fonfria, Robert Gleave, Stefan Senger, Katharine Laura Collis, Andrew P. Moses, Sue D. Collins, Muna H. Abdi, Paul John Beswick, Clarisse L. Lejeune, David Kenneth Dean, Alexander J. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5080-5084
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a3ff37009bb76b9bfd50c27c623c06d
https://doi.org/10.1016/j.bmcl.2010.07.033
https://doi.org/10.1016/j.bmcl.2010.07.033
Autor:
Beverley Smith, Alessandra Gaiba, Jon Graham Anthony Steadman, Penelope C. Staton, Antoinette Naylor, David Matthew Wilson, Robert P. Davis, Susannah Davies, Tania O. Stean, Alastair D. Reith, Mark James Bamford, Christopher A. Parr, David Kenneth Dean, Frank D. King, Andrew K. Takle, Elaine A. Irving, Alison M. Ray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4373-4376
Modification of the potent imidazole-based B-Raf inhibitor SB-590885 resulted in the identification of a series of furan-based derivatives with enhanced CNS penetration. One such compound, SB-699393 (17), was examined in vivo to challenge the hypothe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af69a9ad5d1b9c75f481ac4e3fb01bc5
https://doi.org/10.1016/j.bmcl.2008.06.070
https://doi.org/10.1016/j.bmcl.2008.06.070
Autor:
James T. Townsend, Alessandra Gaiba, David Kendall Jung, Christopher A. Parr, John D. Harling, David Matthew Wilson, Mark James Bamford, Stephen L. Garland, Susannah Davies, Nicholas Bailey, Jason Witherington, Michael J. Alberti, Andrew K. Takle, David Kenneth Dean, Jon Graham Anthony Steadman, Terence A. Panchal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3402-3406
A novel series of imidazo[4,5-c]pyridines bearing a 1,2,5-oxadiazol-3-ylamine functionality has been developed. These are potent inhibitors of mitogen and stress-activated protein kinase-1.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03a34ec33bd554df8f96b52fc1d339b5
https://doi.org/10.1016/j.bmcl.2005.05.021
https://doi.org/10.1016/j.bmcl.2005.05.021
Autor:
Mark James Bamford, Andrew R. Calver, David Matthew Wilson, Rebecca K. Davis, Nicholas Bailey, Isabel Jm Beresford, Jason Witherington, Susannah Davis, Jon Graham Anthony Steadman, Phillip Jeffrey, Vicky Holland, Joanne Schogger, Christopher A. Parr, Jeffrey Wald, Teresa Heslop, Michael A. Briggs, Terrance A. Panchal, Leanne Harris, Andrew D. Medhurst, Kim Brackenborough, David Kenneth Dean, Tania O. Stean, Brenda K. Trail, Nigel Quashie, Angela Worby, Stephen J. Brough, Barry Crook, James Apps, Andrew K. Takle, Robert P. Davis, Sanjeet Singh Sehmi
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(24)
This Letter describes the discovery of GSK189254 and GSK239512 that were progressed as clinical candidates to explore the potential of H3 receptor antagonists as novel therapies for the treatment of Alzheimer's disease and other dementias. By careful
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e541fa0f8606fd8aa20c773c236c2d64
https://pubmed.ncbi.nlm.nih.gov/24269482
https://pubmed.ncbi.nlm.nih.gov/24269482
Autor:
Angela Worby, Mark James Bamford, David Matthew Wilson, Christopher A. Parr, Susannah Davis, Andrew R. Calver, James Apps, Andrew D. Medhurst, Brenda K. Trail, Andrew K. Takle, David Kenneth Dean, Michael A. Briggs, Tom D. Heightman, Trevor White, Isabel Jm Beresford, Tania O. Stean, Robert P. Davis, Sanjeet Singh Sehmi, Terry Panchal, Leanne Harris, Nigel Quashie, Barry Crook, Jon Graham Anthony Steadman, Jason Witherington, Joanne Schogger, Nicholas Bailey
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(24)
This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and simplifying an early screening hit which rapidly led to the discovery of a novel series of H3 rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34f2df3198c9c47dfcdd310f42a1ed70
https://pubmed.ncbi.nlm.nih.gov/24161834
https://pubmed.ncbi.nlm.nih.gov/24161834
Autor:
Jon Graham Anthony Steadman, Daryl S. Walter, Beverley Smith, Lee Abberley, David Kenneth Dean, Elena Fonfria, Tiziana Scoccitti, Anton D. Michel, Sadhana Patel, Shilina Roman, Robert Gleave, Katharine Laura Collis, Stephen J. Medhurst, Andrew P. Moses, Aude Bebius, Paul John Beswick, Andy Billinton
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(22)
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X(7) antagonist with very low in vivo clearance and high oral bioavailabilit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cdb4b6ee4ecb8615e490657bc2ef801
https://pubmed.ncbi.nlm.nih.gov/20934331
https://pubmed.ncbi.nlm.nih.gov/20934331
Autor:
Kim Winborn, Nicola Shuker, Benjamin R. Bellenie, Fiona McKay, Robert W. Ward, Andrew K. Takle, N. Paul King, Sharon Butler, Alessandra Gaiba, Jon Graham Anthony Steadman, Katharine Laura Collis, Jason Witherington, Rio Boatman, Tom D. Heightman, Lee Abberley, David Kenneth Dean, Alison I. Muir, Gareth J. Sanger
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(3)
As part of an on-going lead optimisation effort, a cross screening exercise identified an aryl sulphonyl amide hit that was optimised to afford a highly potent series of ghrelin receptor agonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c4f34f29948982ea29b7786568744f8
https://pubmed.ncbi.nlm.nih.gov/19128969
https://pubmed.ncbi.nlm.nih.gov/19128969
Autor:
Graham Wadsworth, Jon Graham Anthony Steadman, Nicola Shuker, Lee Abberley, Michael A. Briggs, Helmut Kraus, N. Paul King, Tom D. Heightman, David Kenneth Dean, Katharine Laura Collis, Andrew K. Takle, Kim Winborn, Jason Witherington, Gareth J. Sanger, Fiona McKay, Sharon Butler, Alessandra Gaiba, Alison I. Muir
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(6)
A series of small molecule orally bioavailable ghrelin receptor agonists have been identified through systematic optimisation of a high throughput screening hit.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28c166c3676ce1f0ac11de92a47952ea
https://pubmed.ncbi.nlm.nih.gov/18316188
https://pubmed.ncbi.nlm.nih.gov/18316188
Autor:
David Matthew Wilson, Mark James Bamford, Christopher A. Parr, Jason Witherington, James T. Townsend, Terence A. Panchal, Stephen L. Garland, Alessandra Gaiba, Andrew K. Takle, David Kenneth Dean, David Kendall Jung, Susannah Davies, Nicholas Bailey, John D. Harling, Michael J. Alberti, Jon Graham Anthony Steadman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1151
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::74559f0b7518a9fcc3398f2db852dace
https://doi.org/10.1016/j.bmcl.2014.10.001
https://doi.org/10.1016/j.bmcl.2014.10.001
Autor:
Peter J. Lovell, Andrew K. Takle, Gerraint Francis, Jon Graham Anthony Steadman, Murray J. B. Brown, Alexander Hird, Frank D. King, Alastair D. Reith, Susannah Davies, David Kenneth Dean, David Matthew Wilson, Alessandra Gaiba, Antoinette Naylor
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(2)
A novel triarylimidazole derivative, SB-590885 (33), bearing a 2,3-dihydro-1H-inden-1-one oxime substituent has been identified as a potent and extremely selective inhibitor of B-Raf kinase.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d55c7eb4f795bf7976ba678edeb58727
https://pubmed.ncbi.nlm.nih.gov/16260133
https://pubmed.ncbi.nlm.nih.gov/16260133