Zobrazeno 1 - 10
of 548
pro vyhledávání: '"C C, LUCAS"'
Publikováno v:
European Journal of Organic Chemistry. 2022
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2b050546e4def162f16d714b305d4dbf
https://doi.org/10.1002/ejoc.202200684
https://doi.org/10.1002/ejoc.202200684
Autor:
S. Paul Jones, James D. Firth, Mary C. Wheldon, Masakazu Atobe, Roderick E. Hubbard, David C. Blakemore, Claudia De Fusco, Simon C. C. Lucas, Stephen D. Roughley, Lewis R. Vidler, Maria Ann Whatton, Alison J.-A. Woolford, Gail L. Wrigley, Peter O'Brien
Publikováno v:
RSC medicinal chemistry. 13(12)
Fragment-based drug discovery is now widely adopted for lead generation in the pharmaceutical industry. However, fragment screening collections are often predominantly populated with flat, 2D molecules. Herein, we report the synthesis of piperidine-b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::506a35ff9f31d56c1344c52cbe76d494
https://pubmed.ncbi.nlm.nih.gov/36545433
https://pubmed.ncbi.nlm.nih.gov/36545433
Autor:
Simon C. C. Lucas, Ulf Börjesson, Mark J. Bostock, John Cuff, Fredrik Edfeldt, Kevin J. Embrey, Per-Olof Eriksson, Andrea Gohlke, Anders Gunnarson, Michael Lainchbury, Alexander G. Milbradt, Rachel Moore, Philip B. Rawlins, Ian Sinclair, Christopher Stubbs, R. Ian Storer
Publikováno v:
RSC Med Chem
Fragment based drug discovery is a critical part of the lead generation toolbox and relies heavily on a readily available, high quality fragment library. Over years of use, the AstraZeneca fragment set had become partially depleted and instances of c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::446ddff84fa8641f08a20b101425dc2e
https://europepmc.org/articles/PMC9491351/
https://europepmc.org/articles/PMC9491351/
Autor:
Jennifer E. Nelson, Simon C. C. Lucas, Iacovos N Michaelides, Matthias R. Bauer, Benjamin C Whitehurst, R. Ian Storer, Paolo Di Fruscia
Publikováno v:
RSC Med Chem
Aliphatic three- and four-membered rings including cyclopropanes, cyclobutanes, oxetanes, azetidines and bicyclo[1.1.1]pentanes have been increasingly exploited in medicinal chemistry for their beneficial physicochemical properties and applications a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f297b29e4248cacc143b0578d2195082
https://doi.org/10.1039/d0md00370k
https://doi.org/10.1039/d0md00370k
Autor:
Ian D. Wall, Thomas Grimes, Laurie J. Gordon, James Michael Woolven, Simon Taylor, Robert P. Davis, Simon C. C. Lucas, Chun-wa Chung, James J R Gray, Paola Grandi, Nicholas C. O. Tomkinson, Rab K. Prinjha, Robert J. Watson, Inmaculada Rioja, Alex Preston, Alexander N Phillipou, Stephen John Atkinson, Emmanuel Hubert Demont
Herein, a series of 2,3-dihydrobenzofurans have been developed as highly potent bromo and extra-terminal domain (BET) inhibitors with 1000-fold selectivity for the second bromodomain (BD2) over the first bromodomain (BD1). Investment in the developme
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::547bee46f66a5c9178b4a1bb02762f95
https://strathprints.strath.ac.uk/78085/1/Lucas_etal_JMC_2021_Optimization_of_a_series_of_2_3_dihydrobenzofurans_as_highly_potent_second_bromodomain.pdf
https://strathprints.strath.ac.uk/78085/1/Lucas_etal_JMC_2021_Optimization_of_a_series_of_2_3_dihydrobenzofurans_as_highly_potent_second_bromodomain.pdf
Autor:
Chun-wa Chung, Rab K. Prinjha, Simon C. C. Lucas, Nicholas C. O. Tomkinson, Alexander N Phillipou, Stephen John Atkinson, Darren Jason Mitchell, Paul Bamborough, Robert J. Sheppard, Emmanuel Hubert Demont, Robert J. Watson, Laurie J. Gordon, Heather A. Barnett
Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc) histone substrate through key interactions with conserved asparagine and tyrosine residues within the binding pocket. Herein we report the optimization of a ser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5846b0ef827565f0ccfd4008efb5659
https://strathprints.strath.ac.uk/73265/1/Lucas_etal_JMC_2020_The_optimisation_of_potent_ATAD2_and_CECR2_Bromodomain_inhibitors_with_an_atypical_binding_mode.pdf
https://strathprints.strath.ac.uk/73265/1/Lucas_etal_JMC_2020_The_optimisation_of_potent_ATAD2_and_CECR2_Bromodomain_inhibitors_with_an_atypical_binding_mode.pdf
Autor:
Cassie Messenger, Laurie J. Gordon, Simon C. C. Lucas, Aaron T. Cheng, Kelly M Gatfield, John P. Evans, Emma J. Jones, Mahnoor Mahmood, Charles S. Lay, Charlotte E. Carver, Douglas Sammon, Antonia J. Lewis, Alexander N Phillipou, Syandan Chakraborty, Luke A Greenhough, Peter D. Craggs, David J Brierley
Publikováno v:
SLAS discovery : advancing life sciences RD. 25(2)
Malfunctions in the basic epigenetic mechanisms such as histone modifications, DNA methylation, and chromatin remodeling are implicated in a number of cancers and immunological and neurodegenerative conditions. Within GlaxoSmithKline (GSK) we have ut
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc63556b946b71c8a1576c30413bb503
https://pubmed.ncbi.nlm.nih.gov/31875412
https://pubmed.ncbi.nlm.nih.gov/31875412
Autor:
Alan R. Kennedy, Stephen John Atkinson, Matthew Campbell, Stuart C. Davidson, Nicholas C. O. Tomkinson, Simon C. C. Lucas, Carla Alamillo-Ferrer, Jonathan M. Curle
Publikováno v:
The Journal of Organic Chemistry. 83:6728-6740
Treatment of homoallylic N-tosyl amines or allylic N-tosyl hydroxylamines with 1.5 equiv of a malonoyl peroxide provides a stereoselective method to access functionalized pyrrolidines and isoxazolidines. This metal free alkene oxyamination proceeds i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e1970ed5d9e5e7f4e104eae930d4160
https://doi.org/10.1021/acs.joc.8b00392
https://doi.org/10.1021/acs.joc.8b00392
Autor:
Andrew D. Roberts, Peter Francis, Paola Grandi, Emma J. Jones, David P. Dixon, Robert J. Watson, Christina Rau, Peter Pogány, Angela Bridges, Chun-wa Chung, Darren Jason Mitchell, Rab K. Prinjha, Peter D. Craggs, Kelly Locke, Emmanuel Hubert Demont, Anne-Marie Michon, Bhumika Karamshi, Rebecca C. Furze, Paul Bamborough, Robert J. Sheppard, Simon C. C. Lucas, Ana Maria Roa
Publikováno v:
Journal of medicinal chemistry. 62(16)
The bromodomain of ATAD2 has proved to be one of the least-tractable proteins within this target class. Here, we describe the discovery of a new class of inhibitors by high-throughput screening and show how the difficulties encountered in establishin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f80874ffd274bf81cab3a201c3f2f1c
https://pubmed.ncbi.nlm.nih.gov/31398032
https://pubmed.ncbi.nlm.nih.gov/31398032
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3de3bffe208b4378906d5950e2d3a8f1
https://doi.org/10.1016/j.tetlet.2016.09.029
https://doi.org/10.1016/j.tetlet.2016.09.029