Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Sophie M. Bertrand"'
Autor:
Giovanna Bergamini, Stefano Livia, Kenneth David Down, Marcus Bantscheff, Nick Barton, Friedrich B M Reinhard, Paola Grandi, Daniel Thomas, David N. Mallett, Paul Martin Gore, Sophie M. Bertrand, Z.A. Henley, Edith M. Hessel, James E. Rowedder, Mark Price, J. Nicole Hamblin, Birgit Dümpelfeld, Augustin Amour, Steve Keeling, Christina Rau, Máire A. Convery, Chris D. Edwards, Jonathan A. Taylor, Paul Rowland, Aoife C. Maxwell
Publikováno v:
Journal of Medicinal Chemistry. 63:638-655
Optimization of a lead series of PI3Kδ inhibitors based on a dihydroisobenzofuran core led to the identification of potent, orally bioavailable compound 19. Selectivity profiling of compound 19 showed similar potency for class III PI3K, Vps34, and P
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee509ec4ce8051c7f53718e7e95b2637
https://doi.org/10.1021/acs.jmedchem.9b01585
https://doi.org/10.1021/acs.jmedchem.9b01585
Autor:
Paul Scott-Stevens, Qin Donghui, Allen Oliff, Andrew N. Hobbs, Yoshiaki Washio, Josh Cottom, Jennifer A. Borthwick, Julia Coggins, Robert J. Young, Biju Mangatt, Jordi Munoz-Muriedas, Paris Ward, Siegfried B. Christensen, Helen L. Evans, Jingsong Yang, Nino Campobasso, Graham L. Simpson, Julien Chabanet, Xuan Hong, Sophie M. Bertrand, Susan Chen, Helen C. Dawson
Publikováno v:
Journal of Medicinal Chemistry. 62:2154-2171
Abelson kinase (c-Abl) is a ubiquitously expressed, nonreceptor tyrosine kinase which plays a key role in cell differentiation and survival. It was hypothesized that transient activation of c-Abl kinase via displacement of the N-terminal autoinhibito
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64687f04df163cae0b9f2c6dc35de00e
https://doi.org/10.1021/acs.jmedchem.8b01872
https://doi.org/10.1021/acs.jmedchem.8b01872
Publikováno v:
Chemical Science. 10:10412-10416
The challenges of developing sustainable methods of carbon-carbon bond formation remains a topic of considerable importance in synthetic chemistry. Capitalizing on the highly reactive nature of the nitrile imine 1,3-dipole, we have developed a novel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80e68cfac329c6e0a0f35c0aa469e98d
https://doi.org/10.1039/c9sc03032h
https://doi.org/10.1039/c9sc03032h
Autor:
Nicholas C. O. Tomkinson, Sophie M. Bertrand, Kenneth David Down, Brett Cosgrove, Michael David Barker
Physicochemical properties, such as solubility, are important when prioritising compounds for progression on a drug discovery project. There is limited literature around the systematic effects of core changes on thermodynamic solubility. This work de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb089decaaa92b634c134279b6dc9737
https://strathprints.strath.ac.uk/76856/1/Cosgrove_etal_BMCL_2021_Investigating_the_effects_of_the_core_nitrogen_atom_configuration.pdf
https://strathprints.strath.ac.uk/76856/1/Cosgrove_etal_BMCL_2021_Investigating_the_effects_of_the_core_nitrogen_atom_configuration.pdf
Publikováno v:
Chemistry (Weinheim an Der Bergstrasse, Germany)
A range of 1,3,4‐oxadiazoles have been synthesized using a UV‐B activated flow approach starting from carboxylic acids and 5‐substituted tetrazoles. The application of UV light represents an attractive alternative to the traditional thermolytic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa5f3bd88ff244d9f63dec5be7e95a5e
https://strathprints.strath.ac.uk/73628/7/Green_etal_CEJ_2020_UV_induced_1_3_4_oxadiazole_formation_from_5_substituted_tetrazoles.pdf
https://strathprints.strath.ac.uk/73628/7/Green_etal_CEJ_2020_UV_induced_1_3_4_oxadiazole_formation_from_5_substituted_tetrazoles.pdf
Publikováno v:
Chemistry (Weinheim an Der Bergstrasse, Germany)
The need for alternative, complementary approaches to enable C−C bond formation within organic chemistry is an on‐going challenge in the area. Of particular relevance are transformations that proceed in the absence of transition‐metal reagents.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2b0f9d11c22480ded1678bbeec3aa4c
https://strathprints.strath.ac.uk/72437/13/Livingstone_etal_CAEJ_2020_Transition_metal_free_coupling_of_1_3_dipoles_and_boronic.pdf
https://strathprints.strath.ac.uk/72437/13/Livingstone_etal_CAEJ_2020_Transition_metal_free_coupling_of_1_3_dipoles_and_boronic.pdf
Publikováno v:
The Journal of Organic Chemistry
2,5-Diaryltetrazoles are a diverse range of compounds of considerable interest within the field of photochemistry as a valuable precursor of the nitrile imine 1,3-dipole. Current literature approaches toward this heterocycle remain unsuitable for the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3b258dbed36e34b813cec8c3d0e29cf
https://pubmed.ncbi.nlm.nih.gov/32392054
https://pubmed.ncbi.nlm.nih.gov/32392054
Publikováno v:
Wang, G-W, Boyd, O, Young, T A, Bertrand, S M & Bower, J F 2020, ' Rhodacyclopentanones as Linchpins for the Atom Economical Assembly of Diverse Polyheterocycles ', Journal of the American Chemical Society, vol. 142, no. 4, pp. 1740-1745 . https://doi.org/10.1021/jacs.9b12421
Journal of the American Chemical Society
Journal of the American Chemical Society
We outline a conceptual blueprint that provides direct and atom economical access to a wide range of complex polyheterocycles. Our method capitalizes on the ambiphilic reactivity of rhodacyclopentanones that arise upon exposure of cyclopropanes to Rh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a462355f0b696836acc3b0f93eee4fe0
https://research-information.bris.ac.uk/en/publications/a24c8106-0f10-4c30-8814-f0b2af1ac4f1
https://research-information.bris.ac.uk/en/publications/a24c8106-0f10-4c30-8814-f0b2af1ac4f1
Autor:
Olga O. Sokolova, Adam D. J. Calow, Olivia Boyd, Gang-Wei Wang, John F. Bower, Sophie M. Bertrand
Publikováno v:
Boyd, O, Wang, G-W, Sokolova, O O, Calow, A D J, Bertrand, S M & Bower, J F 2019, ' Modular Access to Eight-Membered N-Heterocycles by Directed Carbonylative C-C Bond Activation of Aminocyclopropanes ', Angewandte Chemie-International Edition . https://doi.org/10.1002/anie.201910276
Angewandte Chemie International Edition
Angewandte Chemie International Edition
Aminocyclopropanes equipped with pendant nucleophiles undergo carbonylative heterocyclization triggered by C-C bond activation to generate eight-membered N-heterocycles. In these processes, intramolecular "capture" of a rhodacyclopentanone intermedia
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f8b5b29f98a74f44cb2baf8eee60e03
https://pubmed.ncbi.nlm.nih.gov/31585028
https://pubmed.ncbi.nlm.nih.gov/31585028
Autor:
Colin J. Suckling, Claus Spitzfaden, Andrew N. Hobbs, Craig Jamieson, Peter Francis, Robert J. Young, Ian Churcher, Sophie M. Bertrand, Ryan P. Bingham, Sarah E. Smith, Donald O. Somers, Nicolas Ancellin, Nerina Dodic, Paul S. Carter, Chun-wa Chung, Charlène Fournier, Jennifer A. Borthwick, Stephen D. Pickett
Inhibitors of mitochondrial branched chain aminotransferase (BCATm), identified using fragment screening, are described. This was carried out using a combination of STD-NMR, thermal melt (Tm), and biochemical assays to identify compounds that bound t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::019a009ff86efad911c0ace056f53ba5
https://strathprints.strath.ac.uk/55944/1/Borthwick_etal_JMC_2016_structurally_diverse_mitochondrial_branched_chain_aminotransferase_BCATm_leads_with_varying_binding_modes_identified_by_fragment_screening.pdf
https://strathprints.strath.ac.uk/55944/1/Borthwick_etal_JMC_2016_structurally_diverse_mitochondrial_branched_chain_aminotransferase_BCATm_leads_with_varying_binding_modes_identified_by_fragment_screening.pdf