Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Scott G. Lamont"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1fb6661980000927d0d6487a63f5ff66
https://doi.org/10.1055/s-0040-1719873
https://doi.org/10.1055/s-0040-1719873
Publikováno v:
Advanced Synthesis & Catalysis. 362:2503-2509
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::da22faf3a8c907fb57b06fb8298846ce
https://doi.org/10.1002/adsc.202000134
https://doi.org/10.1002/adsc.202000134
Autor:
Rodrigo J. Carbajo, S. Harlfinger, Lyman Feron, Jason Grant Kettle, E.S. Gleave, Hilary J. Lewis, L. Liu, A. Jackson, Doyle Joseph Cassar, Sharanjeet Kaur Bagal, David Robinson, Radoslaw Polanski, L. Zhang, M.R. Howard, Sabina Cosulich, L. Evans, Jason Breed, Graeme R. Robb, A. Chakraborty, Rachel L. Howells, Rebecca Whiteley, Scott G. Lamont, Lyndsey Hanson, J.K. Kingston, Michael Davies, Iain A. Cumming, Sarah Ross, Sue Bickerton, Paul D. Kemmitt, Derek Ogg, Andrew John Eatherton, James M. Smith, S. Li, Bodnarchuk, Frederick W. Goldberg, Christopher R. Phillips, X. Zhao, Jun Yang, Michael Tonge, Shaun M. Fillery
Publikováno v:
Journal of Medicinal Chemistry. 63:4468-4483
Attempts to directly drug the important oncogene KRAS have met with limited success despite numerous efforts across industry and academia. The KRASG12C mutant represents an "Achilles heel" and has recently yielded to covalent targeting with small mol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0c0d1227f159830cde7d87c48972047a
https://doi.org/10.1021/acs.jmedchem.9b01720
https://doi.org/10.1021/acs.jmedchem.9b01720
Autor:
Scott G. Lamont, Robert D. M. Davies, Christopher J. Morrow, Thomas A. Moss, Andrew Lister, Eric Gangl, Rodrigo J. Carbajo, Paul R. J. Davey, Craig S. Donald, James S. Scott, Tony Johnson, Sébastien L. Degorce, Jon Curwen, Mandy Lawson, Sam D. Groombridge, David Buttar, Radoslaw Polanski, Ryan Greenwood, Andrew Bailey, Jennifer H. Pink
Publikováno v:
Journal of Medicinal Chemistry. 62:1593-1608
Herein, we report the identification and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen receptor degrader antagonists. Replacement of a phenol, present in our previously reported tetrahydroisoquinoline scaffold, w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3c4372ee1b0b56453fd933c416388e4
https://doi.org/10.1021/acs.jmedchem.8b01837
https://doi.org/10.1021/acs.jmedchem.8b01837
Publikováno v:
Tetrahedron Letters. 59:4509-4513
In the following communication we report two complementary approaches for the synthesis of trans 8-substituted-6-phenyl-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolines. The first method, directly from α-methyl substituted indazole ethanamines, wa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a5c019afe8d6e0b4d78b2c35b0488234
https://doi.org/10.1016/j.tetlet.2018.11.021
https://doi.org/10.1016/j.tetlet.2018.11.021
Autor:
Paul D. Kemmitt, Matthew Gill, David W. Watson, Iain Simpson, Mihai V. Popescu, Scott G. Lamont
Publikováno v:
Tetrahedron Letters. 59:4479-4482
2,6-Lutidine has been identified as a beneficial additive for the oxidative cleavage of olefins to ketones by NaIO4 in the presence of catalytic RuCl3, improving the yield and shortening the reaction times. In the absence of 2,6-lutidine reactions st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::03a6b621a582fb0d6cd6018e4529c0de
https://doi.org/10.1016/j.tetlet.2018.11.013
https://doi.org/10.1016/j.tetlet.2018.11.013
Autor:
Keith Dillman, J. Elizabeth Pease, James E. Dowling, Nichola L. Davies, Rana Anjum, Robert D. M. Davies, Janet D. Culshaw, David R. Perkins, Dedong Wu, Julian A. Hudson, Sébastien L. Degorce, Jennifer H. Pink, Nicola Lindsay, Christopher Thomas Halsall, James S. Scott, Scott G. Lamont, Minhui Shen, Andrew D. Ferguson, Alan Rosen, Lisa Drew, Stacey Marden, Claire McWhirter, Sam D. Groombridge, Michele Mayo, Graeme R. Robb
Publikováno v:
Journal of Medicinal Chemistry. 60:10071-10091
Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal structures and structure based design to identify and optimize our scaffold. Compound 28 demonstra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7d9445739130c614b1133a78291bf074
https://doi.org/10.1021/acs.jmedchem.7b01290
https://doi.org/10.1021/acs.jmedchem.7b01290
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38373a373ad6edeea8ce9e1a2378dbce
https://doi.org/10.1021/acs.jmedchem.7b00267
https://doi.org/10.1021/acs.jmedchem.7b00267
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68575e1f1cd6f592b8ead892c32d4cc6
https://pubmed.ncbi.nlm.nih.gov/31710489
https://pubmed.ncbi.nlm.nih.gov/31710489
Autor:
Joe Patel, Mark A. Graham, Maureen Hattersley, Stephen Stokes, David Whittaker, Carr Gregory Richard, David Whalley, Edwin Clark, Craig A. Roberts, Gail L. Wrigley, Alfred A. Rabow, Graeme Walker, Christopher R. Jones, Natalie Stratton, Michael J. Waring, Rowena Callis, Lyman Feron, Robert Hugh Bradbury, Steve C. Glossop, Huawei Chen, Lara Ward, Anil Patel, Gilles Ouvry, Scott G. Lamont
Publikováno v:
Journal of Medicinal Chemistry. 59:7801-7817
Here we report the discovery and optimization of a series of bivalent bromodomain and extraterminal inhibitors. Starting with the observation of BRD4 activity of compounds from a previous program, the compounds were optimized for BRD4 potency and phy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5c6c7a1841e4b9e6991aa022e6aedcc0
https://doi.org/10.1021/acs.jmedchem.6b00070
https://doi.org/10.1021/acs.jmedchem.6b00070