Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Benoit Carbain"'
Autor:
Benoit Carbain, Keisha Hearn, Ildiko Maria Buck, Burcu Anil, Sarah J. Cully, Gianni Chessari, Jane A. Endicott, John Lunec, Neil T. Thompson, Juan Castro, Roger J. Griffin, Rhian S. Holvey, Karen Haggerty, Charlotte H. Revill, Ruth H. Bawn, Stephen R. Wedge, Christiane Riedinger, Christopher N. Johnson, Bernard T. Golding, Lynsey Fazal, Ian R. Hardcastle, Mladen Vinkovic, Claire E. Jennings, Jong Sook Ahn, Bian Zhang, Pamela A. Williams, Celine Cano, Suzannah J. Harnor, Ben Cons, Stephen J. Hobson, E. Anscombe, Jeffrey D. St. Denis, Steven Howard, David R. Newell, Emiliano Tamanini, Nicola E. Wilsher, Miller Duncan Charles, Huw D. Thomas, Timothy J. Blackburn, Martin E.M. Noble, Judith Reeks, Yan Zhao, Luke Bevan
Publikováno v:
Journal of Medicinal Chemistry. 64:4071-4088
Inhibition of murine double minute 2 (MDM2)-p53 protein-protein interaction with small molecules has been shown to reactivate p53 and inhibit tumor growth. Here, we describe rational, structure-guided, design of novel isoindolinone-based MDM2 inhibit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd2c962765a3d64c4d7d02d50fd31b0d
https://doi.org/10.1021/acs.jmedchem.0c02188
https://doi.org/10.1021/acs.jmedchem.0c02188
Autor:
Kathy Boxall, Mangaleswaran Sivaprakasam, David P. Turner, Roger J. Griffin, Corine Mas-Droux, Benoit Carbain, Bernard T. Golding, Richard Bayliss, Ian R. Hardcastle, Mark W. Richards, Andrew M. Fry, Christopher R. Coxon, David R. Newell, Celine Cano, Suzannah J. Harnor, Christopher J. Matheson
Publikováno v:
RSC Medicinal Chemistry
Renewed interest in covalent inhibitors of enzymes implicated in disease states has afforded several agents targeted at protein kinases of relevance to cancers.
Renewed interest in covalent inhibitors of enzymes implicated in disease states has
Renewed interest in covalent inhibitors of enzymes implicated in disease states has
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae2f8ee1ed869eeee706983439e40721
https://pubmed.ncbi.nlm.nih.gov/33479670
https://pubmed.ncbi.nlm.nih.gov/33479670
Publikováno v:
The Journal of Organic Chemistry. 83:15380-15405
3,4-Substituted-5-aminopyrazoles and 4-substituted-2-aminothiazoles are frequently used intermediates in medicinal chemistry and drug discovery projects. We report an expedient flexible synthesis of 3,4-substituted-5-aminopyrazoles (35 examples), bas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c6759b45f3f43358575e3c0e7fb4a74
https://doi.org/10.1021/acs.joc.8b02655
https://doi.org/10.1021/acs.joc.8b02655
Autor:
Benoit Carbain, E. Anscombe, Jane A. Endicott, Christopher R. Coxon, Mathew P. Martin, Stephen R. Wedge, Christopher Wong, Svitlana Korolchuk, Mangaleswaran Sivaprakasam, Bernard T. Golding, Lisa K. Harlow, Celine Cano, Suzannah J. Harnor, Christopher J. Matheson, Lan Z. Wang, David M. Turner, Martin E.M. Noble, David R. Newell, Ian R. Hardcastle, Roger J. Griffin, Susan J. Tudhope
Publikováno v:
Journal of Medicinal Chemistry
Purines and related heterocycles substituted at C-2 with 4’-sulfamoylanilino and at C-6 with a variety of groups have been synthesized with the aim of achieving selectivity of binding to CDK2 over CDK1. 6-Substituents that favour competitive inhibi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e79c5e8c85af8caa2cdd1125fa18b4b
http://europepmc.org/articles/PMC6111440
http://europepmc.org/articles/PMC6111440
Publikováno v:
Advanced Synthesis & Catalysis. 358:701-706
We describe a practical (time-efficient, with commercially available building blocks, user friendly reaction conditions, high purity of products) synthesis of pharmacologically relevant quinoxalinones with three points of diversification that takes a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d55814d73736e8d1258ca02a0996e2ec
https://doi.org/10.1002/adsc.201500826
https://doi.org/10.1002/adsc.201500826
Autor:
Michaela Hylsová, Jindřich Fanfrlík, Kamil Paruch, Martin Lepšík, Pathik S. Brahmkshatriya, Aude Echalier, Vladimír Kryštof, Lenka Musilová, Benoit Carbain, Pavel Hobza, Radek Jorda, Cemal Köprülüoğlu, Susanta Haldar, Haresh Ajani
We present comprehensive testing of solvent representation in quantum mechanics (QM)-based scoring of protein-ligand affinities. To this aim, we prepared 21 new inhibitors of cyclin-dependent kinase 2 (CDK2) with the pyrazolo[1,5-a]pyrimidine core, w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eff55b4896483e77ca94a2153e7ccba7
https://ora.ox.ac.uk/objects/uuid:43f44ab7-8d22-446e-b571-e7a93d3341d3
https://ora.ox.ac.uk/objects/uuid:43f44ab7-8d22-446e-b571-e7a93d3341d3
Autor:
Miller Duncan Charles, Helen L. Reeves, David R. Newell, Bernard T. Golding, Sari F. Alhasan, Gary S. Beale, Benoit Carbain, Ulrich Baisch, Roger J. Griffin
Publikováno v:
Organicbiomolecular chemistry. 13(18)
Regioselective sulfamoylation of primary hydroxyl groups enabled a 5-step synthesis (overall yield 17%) of the first reported small molecule inhibitor of sulfatase-1 and 2, ((2S,3R,4R,5S,6R)-4,5-dihydroxy-2-methoxy-6-((sulfamoyloxy)methyl)tetrahydro-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e6f431ae2b028b705a0b2929e89be3a
https://pubmed.ncbi.nlm.nih.gov/25858034
https://pubmed.ncbi.nlm.nih.gov/25858034
Publikováno v:
Tetrahedron Letters. 51:2717-2719
We report an efficient synthetic approach to phospha-isosteres of important intermediates of the shikimic acid pathway by the application of the HunsdieckerBarton halodecarboxylation to cyclohexenylcarboxylic acids. As examples, phospha-shikimic acid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::deea82b09a99fdf7df2df99ee5df3d24
https://doi.org/10.1016/j.tetlet.2010.03.044
https://doi.org/10.1016/j.tetlet.2010.03.044
Autor:
E. Anscombe, Bernard T. Golding, David J. Paterson, David R. Newell, Benoit Carbain, Lan Z. Wang, Celine Roche, Celine Cano, Allyson J. Campbell, Aude Echalier, Philip J. Jewsbury, Ian R. Hardcastle, Roger J. Griffin, Jane A. Endicott, Karen Haggerty, Martin E.M. Noble
Publikováno v:
Journal of medicinal chemistry. 57(1)
Evaluation of the effects of purine C-8 substitution within a series of CDK1/2-selective O(6)-cyclohexylmethylguanine derivatives revealed that potency decreases initially with increasing size of the alkyl substituent. Structural analysis showed that
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5f9a74eb70cef5a87c2334ff54cd6ab
https://pubmed.ncbi.nlm.nih.gov/24304238
https://pubmed.ncbi.nlm.nih.gov/24304238
Autor:
Celine Cano, Roger J. Griffin, Honorine Lebraud, Benoit Carbain, Victoria S. Archard, Ulrich Baisch, Ian R. Hardcastle, Christopher R. Coxon, Bernard T. Golding, Christopher J. Matheson, David M. Turner, Carlo M. Bawn, Ross W. Harrington
Publikováno v:
Organicbiomolecular chemistry. 12(1)
Recent studies have shown that irreversible inhibition of Nek2 kinase [(Never in mitosis gene a)-related kinase 2], overexpression of which is observed in several cancers, can be achieved using Michael acceptors containing an ethynyl group, which tar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80fb64f9a1e1835663225ea072b00330
https://pubmed.ncbi.nlm.nih.gov/24213855
https://pubmed.ncbi.nlm.nih.gov/24213855