Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Jane E. Moore"'
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:
Lei Wang, Allan Dishington, Jane E. Moore, Kurt Gordon Pike, Wenlin Shao, Andrew Lister, Anil Patel, Lorraine A. Hassall, Sudhir M. Hande, Jane L. Holmes, Douglas Ferguson, Thomas M. McGuire, Jeffrey G. Varnes, Lin Xue, Chungang Gu, Tieguang Yao, Barlaam Bernard Christophe, Lisa Drew, Janet Hawkins, Liangwei Wu, Chris De Savi, Melissa Vasbinder, Andrew D. Ferguson, Darren Stead, Ujjal Sarkar, Michelle Lamb, Nichole O'Connell, Bin Yang, Alexander Hird
Publikováno v:
Journal of medicinal chemistry. 64(20)
Optimization of a series of azabenzimidazoles identified from screening hit 2 and the information gained from a co-crystal structure of the azabenzimidazole-based lead 6 bound to CDK9 led to the discovery of azaindoles as highly potent and selective
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:
Laksmaiah Gingipalli, Jane E. Moore, Rosemary A. Croft, Barlaam Bernard Christophe, Janet Hawkins, Hai-Jun Zhang, Tao Wang, Anil Patel, Lynsie Almeida, Xiaolan Zheng, Kurt Gordon Pike, Timothy Pontz, Allan Dishington, Stephanos Ioannidis, Xiaoyun Wu, Jeffrey W. Johannes, Lorraine A. Hassall, Jane L. Holmes, Thomas M. McGuire
Publikováno v:
Synthesis. 48:1226-1234
Examples of hydroxymethylated analogues of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones are sparse or non-existent in the scientific
Autor:
Suzanne S. Bowker, Clive Green, Graeme R. Robb, Stephen Stokes, Nathaniel G. Martin, Anne Ertan, David G.A. Morgan, Christopher Sheldon, Alexander G. Dossetter, Robert D. M. Davies, David S. Clarke, Alastair J. H. Brown, William McCoull, Helen Pointon, Jane E. Moore, Mark L. Fenwick, Nicholas John Newcombe, Claire Newton, Jane L. Holmes, David J. Masters, Peter Barton, Jennifer Cameron
Publikováno v:
Journal of Medicinal Chemistry. 57:6128-6140
Ghrelin plays a major physiological role in the control of food intake, and inverse agonists of the ghrelin receptor (GHS-R1a) are widely considered to offer utility as antiobesity agents by lowering the set-point for hunger between meals. We identif
Autor:
Stefan Gerhardt, William McCoull, Jane E. Moore, John Revill, Martin J. Packer, Stephan Krapp, James S. Scott, Nicholas John Newcombe, Derek Ogg, Elaine Kilgour, Amanda Rees, Stefan Steinbacher, Nidhal Selmi, Martin Augustin, Caroline Blake, Anne Ertan, Paul Robert Owen Whittamore
Publikováno v:
Med. Chem. Commun.. 5:57-63
3,3-Di-methyl-azetidin-2-ones were identified as potent and selective 11β-HSD1 inhibitors against the human and mouse forms of the enzyme. Structure guided optimisation of LLE was conducted, utilising a key polar interaction and identifying stereoch
A novel fluorous tagging-detagging strategy has been developed featuring a fluorination as the detagging process; fluorous allylsilanes were prepared by cross-metathesis and subsequently subjected to electrophilic fluorodesilylation; Selectfluor was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce8dc509b20830f7d7127ba0bd82fda4
https://doi.org/10.1039/b804484h
https://doi.org/10.1039/b804484h
Autor:
Véronique Gouverneur, Jerome Declerck, Laurence Carroll, Sophie Boldon, Romain Bejot, Jane E. Moore
The Staudinger ligation of phosphine-substituted thioesters with (18)F-fluoroethylazide has been successfully applied to access (18)F-labelled molecules in radiochemical yields superior to 95%; the first fluorous variant of a Staudinger radio-ligatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfcd7d55bd581d8a1d119e2cee776fd5
https://ora.ox.ac.uk/objects/uuid:b650447f-461c-4608-9240-69cd4ebecbf0
https://ora.ox.ac.uk/objects/uuid:b650447f-461c-4608-9240-69cd4ebecbf0
Halogenated organic compounds are highly sought after in a wide variety of fields, for example synthetic and medicinal chemistry as well as materials science. The supported synthesis of organohalogens has been extensively developed in the field of im
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70ba218a22f759532516c0b3682e330e
https://doi.org/10.1055/s-0031-1289590
https://doi.org/10.1055/s-0031-1289590
Publikováno v:
ChemInform. 47
The first regioselective, mild bromination of thieno[2,3-b]pyridine is described herein. The reaction proceeds with selectivity toward the 4-position (87% isolated yield). Subsequent cross-coupling reactions proceed in excellent yields and demonstrat