Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Gary, Fairley"'
Autor:
Rachel L. Howells, Scott G. Lamont, Thomas M. McGuire, Samantha Hughes, Rachel Borrows, Gary Fairley, Lyman J. L. Feron, Ryan D. R. Greenwood, Eva Lenz, Emma Grant, Iain Simpson
Publikováno v:
Synthesis. 54:2267-2281
As part of a drug discovery program, 4-pyrazin-2-yl-1H-pyrrole-2-carboxamides were accessed along with a number of bicyclic analogues. Routes to these compounds were largely absent from the scientific literature. The synthesis of a 4-(pyrazin-2-yl)-1
Autor:
Edward J. Hennessy, Marianne Schimpl, Emma Rivers, Paul D. Smith, Elizabeth Hardaker, Ann T. Doherty, Nichola L. Davies, Jon Travers, Qianxiu Zhu, Beth Williamson, Graham Smith, Lorraine Mooney, Helen Musgrove, Kristin Goldberg, Muireann Coen, Anne-Laure Lainé, Xiefeng Jiang, Philip Hopcroft, Yuting Zheng, Robert I Troup, George Hodgson, Nicola Lindsay, Lindsay McMurray, Olga Collingwood, Stephen D. Wilkinson, Sharon Tentarelli, Guang He, Philip B. Rawlins, Roshini Markandu, Jon Winter-Holt, Josephine Walton, Ankur Karmokar, J. Willem M. Nissink, Yumeng Mao, Dejian Yang, Alexander Pflug, Gary Fairley, Scott Boyd, Cheng Wang, Anne Jackson, Martin R. Brown, William McCoull, Neville McLean, Venkatesh Pilla Reddy
Publikováno v:
Journal of Medicinal Chemistry. 64:13524-13539
Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncology therapeutics by restoring the innate immune response in the tumor microenvironment. Highly selective dual Mer/Axl kinase inhib
Autor:
David W. Watson, James S. Scott, Coura R. Diène, Shaun M. Fillery, Charlene Fallan, Gary Fairley, Thomas George Christopher Hayhow, Rachel E. A. Borrows
Publikováno v:
Chemistry – A European Journal. 26:16818-16823
A palladium-catalysed Buchwald-Hartwig amination for lenalidomide-derived aryl bromides was optimised using high throughput experimentation (HTE). The substrate scope of the optimised conditions was evaluated for a range of alkyl- and aryl- amines an
Autor:
Michael J. Tucker, Thomas A. Moss, James S. Scott, Barlaam Bernard Christophe, Paul R. J. Davey, Ryan Greenwood, Stephen Stokes, Gary Fairley, Radoslaw Polanski, Holia Hatoum-Mokdad, David Longmire, Eric Gangl, Bin Yang, Andrew Lister, Jeffrey G. Varnes
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition of fluorine on
Autor:
William, McCoull, Scott, Boyd, Martin R, Brown, Muireann, Coen, Olga, Collingwood, Nichola L, Davies, Ann, Doherty, Gary, Fairley, Kristin, Goldberg, Elizabeth, Hardaker, Guang, He, Edward J, Hennessy, Philip, Hopcroft, George, Hodgson, Anne, Jackson, Xiefeng, Jiang, Ankur, Karmokar, Anne-Laure, Lainé, Nicola, Lindsay, Yumeng, Mao, Roshini, Markandu, Lindsay, McMurray, Neville, McLean, Lorraine, Mooney, Helen, Musgrove, J Willem M, Nissink, Alexander, Pflug, Venkatesh Pilla, Reddy, Philip B, Rawlins, Emma, Rivers, Marianne, Schimpl, Graham F, Smith, Sharon, Tentarelli, Jon, Travers, Robert I, Troup, Josephine, Walton, Cheng, Wang, Stephen, Wilkinson, Beth, Williamson, Jon, Winter-Holt, Dejian, Yang, Yuting, Zheng, Qianxiu, Zhu, Paul D, Smith
Publikováno v:
Journal of medicinal chemistry. 64(18)
Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncology therapeutics by restoring the innate immune response in the tumor microenvironment. Highly selective dual Mer/Axl kinase inhib
Publikováno v:
Tetrahedron Letters. 59:3574-3578
A facile synthesis of novel 1,2,6,7-tetrahydro-3 H -pyrazolo[4,3- c ]pyridine-3,4(5 H )-diones has been achieved. The operationally simple procedure, using readily available intermediates, allows for rapid derivatisation of the pharmacophore with alk
Autor:
Jia Tang, Richard A. Ward, Paul A. Bethel, Scott G. Lamont, Julian A. Hudson, Philip Hopcroft, Clifford David Jones, Steve Swallow, Richard J. Lewis, Tomkinson Gary Peter, Baochang Zhai, Nicola Lindsay, Jason Breed, Emma J. Davies, Yongchao Li, Vikki Flemington, Michael Tonge, Paul Farrington, Ryan Greenwood, Mark A. Graham, Linda Sandin, Thomas M. McGuire, James F. McCabe, Mark J. Anderton, Michael R. James, Andrew Hornby Dobson, Philip B. Rawlins, Lyndsey Hanson, Iain Simpson, Karen Roberts, Gary Fairley, Rachel L. Howells, Christopher R. Jones, Calum Cook, Francis D. Gibbons, Zhiqiang Dong, Lyman Feron, Zhenhua Wang
Publikováno v:
Journal of medicinal chemistry. 62(24)
The RAS/MAPK pathway is a major driver of oncogenesis and is dysregulated in approximately 30% of human cancers, primarily by mutations in the BRAF or RAS genes. The extracellular-signal-regulated kinases (ERK1 and ERK2) serve as central nodes within
Autor:
Calum Cook, Tina Howard, Emma J. Davies, Lyman Feron, Jia Tang, Mark A. Graham, Paul A. Bethel, Vikki Flemington, Scott G. Lamont, Judit E. Debreczeni, Gary Fairley, Michael Tonge, Steve St-Gallay, Clifford David Jones, Karen Roberts, Christopher R. Jones, Baochang Zhai, Iain Simpson, Julian A. Hudson, Lyndsey Hanson, Zhenhua Wang, Richard A. Ward, Michael James, Richard J. Lewis, Nicola Griffin, Steve Swallow, Philip Hopcroft, Nicola Lindsay, Ryan Greenwood
Publikováno v:
Journal of Medicinal Chemistry. 60:3438-3450
There are a number of small-molecule inhibitors targeting the RAS/RAF/MEK/ERK signaling pathway that have either been approved or are in clinical development for oncology across a range of disease indications. The inhibition of ERK1/2 is of significa
Autor:
Susan E. Critchlow, Judit E. Debreczeni, Louise Goodwin, Shaun M. Fillery, Gary Fairley, David Whittaker, Nicola Colclough, Richard A. Ward, Mark A. Graham, Catherine Bardelle, Jason Grant Kettle, Kevin Hudson, Sylvie Guichard, Peter Ballard, Mark Cockerill
Publikováno v:
Journal of Medicinal Chemistry. 58:2834-2844
Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response.
Autor:
George W. Weaver, Mark R. J. Elsegood, Simon J. Teat, Gary Fairley, Beatriz Fernandez, Gareth J. Pritchard
Publikováno v:
Tetrahedron Letters. 56(36):5120-5122
An unexpected azeto[2,3-c]quinolizinedione has been isolated during synthetic studies on the base catalyzed condensation of ethyl 6-methylpyridin-2(1H)-on-1-ylacetate with benzil. Closure of a fused four-membered azetidinone ring occurred when potass