Stuart Cockerill
GlaxoSmithKline
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Publication
Featured researches published by Stuart Cockerill.
Bioorganic & Medicinal Chemistry Letters | 2008
Richard Martyn Angell; Tony D. Angell; Paul Bamborough; Mark J. Bamford; Chun-wa Chung; Stuart Cockerill; Stephen Flack; Katherine Louise Jones; Dramane I. Laine; Timothy Longstaff; Steve Ludbrook; Rosannah Pearson; Kathryn J. Smith; Penny A. Smee; Don O. Somers; Ann Louise Walker
The biphenyl amides (BPAs) are a series of p38alpha MAP kinase inhibitors. Compounds are able to bind to the kinase in either the DFG-in or DFG-out conformation, depending on substituents. X-ray, binding, kinetic and cellular data are shown, providing the most detailed comparison to date between potent compounds from the same chemical series that bind to different p38alpha conformations. DFG-out-binding compounds could be made more potent than DFG-in-binding compounds by increasing their size. Unexpectedly, compounds that bound to the DGF-out conformation showed diminished selectivity. The kinetics of binding to the isolated enzyme and the effects of compounds on cells were largely unaffected by the kinase conformation bound.
Bioorganic & Medicinal Chemistry Letters | 2008
Richard Martyn Angell; Nicola Mary Aston; Paul Bamborough; Jacky B. Buckton; Stuart Cockerill; Suzanne J. deBoeck; Chris D. Edwards; Duncan S. Holmes; Katherine Louise Jones; Dramane I. Laine; Shila Patel; Penny A. Smee; Kathryn J. Smith; Don O. Somers; Ann Louise Walker
The biphenyl amides (BPAs) are a novel series of p38alpha MAP kinase inhibitor. The optimisation of the series to give compounds that are potent in an in vivo disease model is discussed. SAR is presented and rationalised with reference to the crystallographic binding mode.
Bioorganic & Medicinal Chemistry | 1999
Martin John Slater; Stuart Cockerill; Robert Baxter; Kam Gohil; Clare Gowrie; J.Edward Robinson; Edward Littler; Nigel R. Parry; Roger W. Randall; Wendy Snowden
In our search for new, safer anti-HCMV agents, we discovered that the natural product Arcyriaflavin A (la) was a potent inhibitor of HCMV replication in cell culture. A series of analogues (symmetrical indolocarbazoles) was synthesised to investigate structure activity relationships in this series against a range of herpes viruses (HCMV, VZV, HSV1, and 2). This identified a number of novel, selective and potent inhibitors of HCMV, 12,13-dihydro-2,10-difluoro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol e-5,7-(6H)-dione (1d) being the best example (IC50=40 nM, therapeutic index > 1450). Compounds described in this series were generally poor inhibitors of protein kinase C betaII, and no correlation was found between the ability to inhibit HCMV and the enzyme PKC.
Bioorganic & Medicinal Chemistry Letters | 2001
Martin John Slater; Robert Baxter; Robert W. Bonser; Stuart Cockerill; Kam Gohil; Nigel R. Parry; Ed Robinson; Roger W. Randall; Clive Leonard Yeates; Wendy Snowden; Adeline Walters
The synthesis and antiviral evaluation of unsymmetrical indolocarbazole derivatives of Arcyriaflavin A, substituted with a range of alkyl groups at the indole nitrogen, is described. Structure-activity relationships in this series against human cytomegalovirus (HCMV) replication in cell culture are reported. Compound 4b was identified as potent inhibitor of HCMV (IC(50)=19 nM), which retained activity against a range of HCMV strains including ganciclovir resistant isolates.
Cancer Research | 2001
David W. Rusnak; Karen Affleck; Stuart Cockerill; Colin Stubberfield; Robert J. Harris; Martin John Page; Kathryn Jane Smith; Stephen Barry Guntrip; Malcolm Clive Carter; Robert Shaw; Amanda Jowett; Jeremy N. Stables; Peter Topley; Edgar R. Wood; Perry S. Brignola; Sue H. Kadwell; Bryan R. Reep; Robert J. Mullin; Krystal J. Alligood; Barry R. Keith; Renae M. Crosby; Doris M. Murray; W. Blaine Knight; Tona M. Gilmer; Karen Elizabeth Lackey
Archive | 2001
Michael John Alberti; Ian Robert Baldwin; Mui Cheung; Stuart Cockerill; Philip A. Harris; David Kendall Jung; Gregory Peckham; Michael Robert Peel; Jennifer Gabriel Badiang; Kirk L. Stevens; James Marvin Veal
Bioorganic & Medicinal Chemistry Letters | 2008
Richard Martyn Angell; Paul Bamborough; Anne Cleasby; Stuart Cockerill; Katherine Louise Jones; Christopher J. Mooney; Donald O. Somers; Ann Louise Walker
Bioorganic & Medicinal Chemistry Letters | 2008
Richard Martyn Angell; Tony D. Angell; Paul Bamborough; David W. Brown; Murray J.B. Brown; Jacky B. Buckton; Stuart Cockerill; Chris D. Edwards; Katherine Louise Jones; Tim Longstaff; Penny A. Smee; Kathryn J. Smith; Don O. Somers; Ann Louise Walker; Malcolm Willson
Archive | 2008
Malcolm Clive Carter; Stuart Cockerill; Stephen Flack; Christopher James Wheelhouse
Antiviral Research | 2010
Malcolm Clive Carter; Bob Baxter; David John Bushnell; Stuart Cockerill; Jo Chapman; Sally Fram; Emma Goulding; Mike Lockyer; Neil Mathews; Pilar Najarro; Dilupa Rupassara; James Iain Salter; Elaine Thomas; Chris Wheelhouse; Jessica Borger; Kenneth L. Powell