Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Peter H. Crackett"'
Autor:
Xingrong Liu, Nico Ghilardi, Simon Charles Goodacre, Michael Siu, Jim Nonomiya, G. Buckley, Adam R. Johnson, Yun-Xing Cheng, F.A. Romero, Nick Ray, Rohan Mendonca, C. Robinson, Yuen Po-Wai, Jane R. Kenny, Marya Liimatta, Terry Kellar, Mark Zak, Gary Salmon, J. Lloyd, D.G. Brown, Neville James Mclean, Joseph P. Lyssikatos, Emily J. Hanan, Patrick J. Lupardus, Pawan Bir Kohli, Christopher A. Hurley, Guiling Zhao, Paul Gibbons, Peter H. Crackett
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1522-1531
Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1, JAK2, and TYK2) to its receptor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5e867a785065ce94ed8447c01ad10c0
https://doi.org/10.1016/j.bmcl.2019.04.008
https://doi.org/10.1016/j.bmcl.2019.04.008
Autor:
Steve, Price, Walter, Bordogna, Richard J, Bull, David E, Clark, Peter H, Crackett, Hazel J, Dyke, Matthew, Gill, Neil V, Harris, Julia, Gorski, Julia, Lloyd, Peter M, Lockey, Julia, Mullett, Alan G, Roach, Fabien, Roussel, Anne B, White
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:370-375
Optimisation of ADS100380, a sub-micromolar HDAC inhibitor identified using a virtual screening approach, led to a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids (6a-i), that possessed significant HDAC inhibitory activity. Sub
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e046b9f8893ae303051b30354b44b450
https://doi.org/10.1016/j.bmcl.2006.10.048
https://doi.org/10.1016/j.bmcl.2006.10.048
Autor:
Guillaume Médard, Stephen P. Schmidt, Raman Narukulla, Emanuela Gancia, Jason Halladay, Sarah Major, Sharon Yee, Brenda Burton, Ping Wu, Lorraine Axford, Simon Charles Goodacre, Michael Flagella, Eileen Mary Seward, Joy Drobnick, Joanne Hewitt, Charles Ellwood, Lewis J. Gazzard, Judi Ramiscal, Samuel Kintz, Matthew Gill, Calum Macleod, Hazel Hunt, Kerry Chapman, Shiva Malek, Peter H. Crackett, Huifen Chen, Christian Wiesmann, Ivana Yen, Jennifer Epler, Karen Williams, Elizabeth Blackwood, Joseph P. Lyssikatos
Publikováno v:
Journal of medicinal chemistry. 58(12)
Checkpoint kinase 1 (ChK1) plays a key role in the DNA damage response, facilitating cell-cycle arrest to provide sufficient time for lesion repair. This leads to the hypothesis that inhibition of ChK1 might enhance the effectiveness of DNA-damaging
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9bfa27960fc92cee387acb5db5e8b8fb
https://pubmed.ncbi.nlm.nih.gov/25988399
https://pubmed.ncbi.nlm.nih.gov/25988399
Autor:
Kathy Barrett, Paul Gibbons, Steven Shia, Jane R. Kenny, Mark Zak, Charles Ellwood, Sharada Labadie, Richard James Bull, Chris Hamman, Peter H. Crackett, Peter Gribling, Peter S. Dragovich, Scott Savage, Jiangpeng Liao, Jason DeVoss, Christine Chang, Paroma Chakravarty, Mercedesz Balazs, Wyne P. Lee, Tony Johnson, Rebecca Pulk, Michael F. T. Koehler, Gauri Deshmukh, Marya Liimatta, Janusz J. Kulagowski, Pawan Bir Kohli, Anne van Abbema, Austin John Reeve, Rohan Mendonca, Adam R. Johnson, Ignacio Aliagas, Simon Gaines, Charles Eigenbrot, Yisong Xiao, Nico Ghilardi, Jing Yang, Christopher A. Hurley, Philippe Bergeron, Wade S. Blair, Peter Hewitt, Stuart Ward, Eric Harstad, Micah Steffek, Barbara Avitabile-Woo, Stefan Gradl, Raman Narukulla, Savita Ubhayakar
Publikováno v:
Journal of medicinal chemistry. 56(11)
Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which provided consistently high levels of selectivity for JAK1 over JAK2 to the imidazopyrrolopyridine series of JAK1 inhibitors. X-ray structures of a C-2 hydroxyethyl a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53d0d607376d7e1e01099fe1e9376df8
https://pubmed.ncbi.nlm.nih.gov/23659214
https://pubmed.ncbi.nlm.nih.gov/23659214
Autor:
Adam R. Johnson, Raman Narukulla, Janusz J. Kulagowski, Robert James Maxey, Rina Fong, Stuart Ward, Wade S. Blair, Hazel Joan Dyke, Jane R. Kenny, Marya Liimatta, Nico Ghilardi, Mark Zak, Patrick J. Lupardus, Christopher A. Hurley, Paul Gibbons, Rebecca Pulk, Richard James Bull, Pawan Bir Kohli, Peter H. Crackett, Christine Chang, Savita Ubhayakar, Anne van Abbema, Peter Hewitt, Bohdan Waszkowycz, Gauri Deshmukh, Tony Johnson, Rohan Mendonca
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(12)
The identification of a novel fused triazolo-pyrrolopyridine scaffold, optimized derivatives of which display nanomolar inhibition of Janus kinase 1, is described. Prototypical example 3 demonstrated lower cell potency shift, better permeability in c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e5dd453bc11f612af005089b1b8eb7f
https://pubmed.ncbi.nlm.nih.gov/23642482
https://pubmed.ncbi.nlm.nih.gov/23642482
Autor:
David J. Bushnell, Joseph A. Martin, Michelle P. Gunn, Stephen J. Dunsdon, Robert W. Lambert, Kevin E. B. Parkes, Andrew C. Freeman, Richard A. Hopkins, Peter H. Crackett
Publikováno v:
The Journal of Organic Chemistry. 59:3656-3664
Ro 31-8959 (1), a potent and selective inhibitor of HIV proteinase, is currently in phase III clinical trials. Six approaches for the large-scale synthesis of this compound have been studied. All routes employ an initial disconnection to an electroph
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::153f097c84eac37b1ee2d4555fd3a8a2
https://doi.org/10.1021/jo00092a026
https://doi.org/10.1021/jo00092a026
Publikováno v:
Tetrahedron Letters. 34:5623-5626
A mild and flexible method for the preparation of bisindolylmaleimides from the corresponding indoles and indole-3-acetimidate esters is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::625683fca03eed1280e135316453b12a
https://doi.org/10.1016/s0040-4039(00)73899-8
https://doi.org/10.1016/s0040-4039(00)73899-8
Publikováno v:
ChemInform. 22
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::30df9b2e277ce2b5cdc25b2a044f950e
https://doi.org/10.1002/chin.199135268
https://doi.org/10.1002/chin.199135268
Publikováno v:
ChemInform. 24
A mild and flexible method for the preparation of bisindolylmaleimides from the corresponding indoles and indole-3-acetimidate esters is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ab23e0c981c97098a72a4036c70e1457
https://doi.org/10.1002/chin.199352169
https://doi.org/10.1002/chin.199352169
Autor:
Robin G. Pritchard, Brian Beagley, Richard J. Stoodley, Peter H. Crackett, Colin W. Greengrass
Publikováno v:
J. Chem. Soc., Perkin Trans. 1. :773-781
t-Butyl hydroxy{4-[(Z)-2-(methoxycarbonyl)vinylthio]-2-oxoazetidin-1-yl}acetate (19a) was transformed into t-butyl 2-endo-methoxycarbonylmethyl-3-thiacepham-4-exo-carboxylate (20a) by sequential reactions involving thionyl chloride, potassium thioace
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dd928d1a8eb91dfbcf6828b25abf9472
https://doi.org/10.1039/p19900000773
https://doi.org/10.1039/p19900000773