Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Calum, Cook"'
Autor:
James Morrison, Rachel H. Munday, Thomas O. Ronson, Matthew R. Tatton, Hucheng Zhao, Calum Cook, Daniël de Bruin, Kevin William Leslie, Kuangchu Dai, David Buttar, Catalina Ferrer, James Douglas
Publikováno v:
The Journal of Organic Chemistry. 87:2075-2086
Route design and proof of concept synthesis was conducted on a synthetically challenging atropisomeric KRASG12C inhibitor to support clinical API manufacture. Improvements to the synthesis of a chiral piperazine fragment gave reduced step count and s
Autor:
Andrew D. Campbell, Staffan Karlsson, Štefan Moravčík, Hanna Leek, Kuangchu Dai, Matthew R. Tatton, Kristina Öhlén, Hucheng Zhao, Marcus Malmgren, Hans Emtenäs, Anna-Carin C. Carlsson, Grigorios Nikitidis, Calum Cook, Anna C. Jonson, Subhash Pithani
Publikováno v:
Organic Process Research & Development. 26:710-729
Autor:
Staffan Karlsson, Helen Benson, Calum Cook, Gordon Currie, Jerome Dubiez, Hans Emtenäs, Janet Hawkins, Rebecca Meadows, Peter D. Smith, Jeffrey Varnes
Publikováno v:
Organic Process Research & Development. 26:601-615
Autor:
Tieguang Yao, Liangwei Wu, Craig S. Donald, Douglas Ferguson, Lei Wang, Andrew Pike, Jianyan Wang, Justin Cidado, Dedong Wu, Kurt Gordon Pike, Kumar Thakur, Chungang Gu, Calum Cook, James Horstick, Tyler Grebe, Theresa Proia, Darren Stead, Alexander Hird, Michelle Lamb, Wenlin Shao, Nichole O'Connell, Yun Jiang, Sudhir M. Hande, Bin Yang, Janet Hawkins, Barlaam Bernard Christophe, Neil Sumner, Melissa Vasbinder, Andrew D. Ferguson, Jane E. Moore, Jeffrey G. Varnes, Bryan Roberts, Maryann San Martin, Lisa Drew, Ujjal Sarkar, Allan Dishington, Chris De Savi, Robert Casella, Steve C. Glossop, Jane L. Holmes, Thomas M. McGuire
Publikováno v:
Journal of Medicinal Chemistry. 63:15564-15590
A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing o
Autor:
James J, Douglas, Matthew R, Tatton, Daniël, de Bruin, David, Buttar, Calum, Cook, Kuangchu, Dai, Catalina, Ferrer, Kevin, Leslie, James, Morrison, Rachel, Munday, Thomas O, Ronson, Hucheng, Zhao
Publikováno v:
The Journal of organic chemistry. 87(4)
Route design and proof of concept synthesis was conducted on a synthetically challenging atropisomeric KRAS
Autor:
Hans Emtenäs, Paul M. Gillespie, Staffan Karlsson, Mubina Mohamed, Calum Cook, Kenny J. H. Fan
Publikováno v:
Organic Process Research & Development. 21:1668-1674
Starting from sodium azide, methyl-bromoacetate, and 3-methylbut-1-yne, a safe and efficient three-step continuous process was developed to obtain 2-(4-isopropyl-1H-1,2,3-triazol-1-yl)acetic acid. Isolation of hazardous intermediates was avoided, and
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:
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:
Anil Patel, Rebecca E. Meadows, Kurt Gordon Pike, Jane E. Moore, Turner Paul, Darren Stead, Barlaam Bernard Christophe, Andrew Stark, Jemma Clark, Janet Hawkins, Bin Yang, Bryan Roberts, Craig S. Donald, Gemma Davison, Esther Moore, Chris De Savi, Tyler Grebe, Calum Cook, Melissa Vasbinder, Simon C. C. Lucas, Andrew Lister, Jeffrey G. Varnes, Kumar Thakur, Sudhir M. Hande, Jane L. Holmes, Thomas M. McGuire, Alexander Hird, Allan Dishington
Publikováno v:
Tetrahedron Letters. 57:4718-4722
As part of a medicinal chemistry program, we adapted known synthetic methods for the late-stage diversification of 2,4-substituted 7-azaindoles. The strengths and weaknesses of these strategies are discussed. In the course of this work, three optimiz
Autor:
Stephan Krapp, James J. Crawford, Lyn Rosenbrier Ribeiro, Andrew David Morley, Jonathan E. Finlayson, Calum Cook, Caroline Smith, Jonathan Bowyer, Anja Jestel, Julian A. Hudson, Stefan Steinbacher, Benjamin P. McDermott, Thomas M. McGuire, Adrian John Highton, Alexander G. Dossetter, Ken Page, Peter W. Kenny, Morris Jeffrey James, Christine Heyes, Philip A. MacFaul, Helen Sawney, Scott W. Martin
Publikováno v:
Journal of Medicinal Chemistry. 55:8827-8837
Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and pharmacokinetics. Compounds with a 3,4-(CH₃O)₂Ph motif, such as 31, were found to have excel