Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Jeremy John Payne"'
Autor:
Xichen Lin, Michael E. Muratore, Huijie Li, Ami S. Lakdawala, Jakob Busch-Petersen, Ruth R. Osborn, David D. Miller, Jeffrey K. Kerns, Rick P. C. Cousins, Ian Robert Baldwin, Paul Bamborough, John Yonchuk, Ann M. Bullion, Lin Guoliang, Jeffrey C. Boehm, Wei Fu, John A. Christopher, Edward F. Webb, Roderick S. Davis, William L. Rumsey, Rita Field, Jeremy John Payne, Hong Nie
Publikováno v:
ACS Medicinal Chemistry Letters. 9:1164-1169
[Image: see text] IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization of a series of 3,5-disubstituted-indole-7-carboxamides for
Autor:
Heather Hobbs, Rick P. C. Cousins, Caroline Whitworth, Ruth R. Osborn, Cesar Ramirez-Molina, Giorgia Vicentini, Chris Ioannou, Chun-wa Chung, Jeremy John Payne, Michelle L. Heathcote, Michael David Barker, Sebastien Andre Campos, Paul Faulder, Mary A. Morse, William L. Rumsey, John Liddle, Daniel Terence Tape, John Martin Pritchard, Rick Williamson, Duncan S. Holmes, Paul Bamborough
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5222-5226
The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good ef
Autor:
Jeremy John Payne, Geoff W. Mellor, Smith Kathryn Jane, Richard A. Williamson, Sebastien Andre Campos, Geoffrey J. Cutler, Caroline Whitworth, Mary A. Morse, Michael David Barker, Heather Hobbs, Rick P. C. Cousins, Duncan S. Holmes, Daniel Terence Tape, Paul Bamborough, John Martin Pritchard, John Liddle, Chris Ioannou
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(9)
The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.
Autor:
Paul F. Lambeth, Fiona S. Lucas, Richard Howard Green, Martin E. Swarbrick, Jeremy John Payne, Lee William Page, Malcolm Clive Carter, Paul John Beswick, Alexander J. Stevens, Sharon C Stratton, Neil Anthony Pegg, John Skidmore, Savvas Kleanthous, Alastair J. Stuart, Sue D. Collins, Sharon Bingham, John Andrew Corfield, Richard Stocker, Joanne O. Wiseman, C. David Hartley, Helen Susanne Price, Neil Mathews, Laura J. Chambers, Iain P. Chessell, Robert Gleave, Nick M. Clayton, Alan Naylor, C. Bountra
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(15)
A novel series of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidine-based cyclooxygenase-2 (COX-2) inhibitors, which have a different arrangement of substituents compared to the more common 1,2-diarylheterocycle based molecules, have bee