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Dive into the research topics where Stuart Cockerill is active.

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Featured researches published by Stuart Cockerill.


Bioorganic & Medicinal Chemistry Letters | 2008

Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes

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

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.

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

Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication.

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

Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication

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

The Characterization of Novel, Dual ErbB-2/EGFR, Tyrosine Kinase Inhibitors: Potential Therapy for Cancer

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

Fused pyrazole derivatives bieng protein kinase inhibitors

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

Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode

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

Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.

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

Heterocyclic derivatives and their use in treating hepatitis c

Malcolm Clive Carter; Stuart Cockerill; Stephen Flack; Christopher James Wheelhouse


Antiviral Research | 2010

Diphenylcarboxamides as Inhibitors of HCV Non-Structural Protein NS5a

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

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