Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Andrew Peter Thomas"'
Autor:
J. Willem M. Nissink, Rongxuan Dou, Gabriele Fumagalli, Andrew Peter Thomas, Rodrigo J. Carbajo, Jonathan Tart, David R. Spring
Publikováno v:
Journal of Medicinal Chemistry. 64:17287-17303
RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identif
Autor:
Ian M. Hardern, Jarrod Walsh, Ed Wheatley, Jon Winter-Holt, Sarita Maman, Judit E. Debreczeni, Graeme Walker, Susan E. Critchlow, Gareth M. Davies, Nicola J. Evans, Richard A. Ward, Neil P. Jones, Sheila B. McLoughlin, Andrew Peter Thomas, Neil Bennett, Geoff Holdgate, Nicola Curtis, Stephen A. St-Gallay, Lindsey Leach, Laurent Rigoreau, Andrew P. Turnbull, Marian Preston
Publikováno v:
SLAS discovery : advancing life sciences RD. 23(1)
A high-throughput screen (HTS) of human 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) resulted in several series of compounds with the potential for further optimization. Informatics was used to identify active chemotypes with lead-l
Autor:
Andrew Peter Thomas, Anne-Kathrin Schott, Jennifer H. Pink, Jason Breed, Karen Roberts, David M. Andrews, Andrew G. Leach, Richard A. Norman, Derek Ogg, Andrew P. Garner, Jonathon P. Orme, David Alan Rudge, Kevin Michael Foote
Publikováno v:
Journal of Medicinal Chemistry. 55:5003-5012
The design of compounds that selectively inhibit a single kinase is a significant challenge, particularly for compounds that bind to the ATP site. We describe here how protein-ligand crystal structure information was able both to rationalize observed
Autor:
Stephen Green, Nicholas John Newcombe, Alexandra McGregor, Catherine Geh, Andrew Peter Thomas, Kate Byth, Andy Barker, Michael A. Walker, Robert W. Wilkinson, Cheryl Forder, Sandra E. Oakes, Gareth D Hughes, Jim Growcott, Clive Green
Publikováno v:
Molecular Cancer Therapeutics. 8:1856-1866
Deregulation of the cell cycle has long been recognized as an essential driver of tumorigenesis, and agents that selectively target key cell cycle components continue to hold promise as potential therapeutics. We have developed AZD5438, a 4-(1-isopro
Autor:
J.J. Stanway, Nicola Cooper, David William AstraZeneca R D Alderley Heaton, Kate Byth, Richard A. Norman, Siân Rowsell, Jason Breed, Claire A. Minshull, Sandra E. Oakes, Janet D. Culshaw, Richard A. Pauptit, Julie A. Tucker, Andrew Peter Thomas, Anna L Valentine, Andrew Pannifer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2249-2252
Modification of imidazo[1,2-a]pyridine CDK inhibitors lead to identification of less lipophilic imidazo[1,2-b]pyridazine series of CDK inhibitors. Although several equivalent compounds from these two series have similar structure and show similar CDK
Autor:
John Maddock, Mary F. Mahon, Kieran C. Molloy, Graham R. Evans, Varinder K. Aggarwal, Martin J. Rice, Andrew Peter Thomas, Richard J. Franklin
Publikováno v:
The Journal of Organic Chemistry. 60:2174-2182
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2615-2620
The synthesis of analogues of tetrahydroquinoline angiotensin II antagonist, ZENECA ZD6888, bearing substituents on the biphenyl ring system is reported. Several of these compounds show comparable or superior activity to ZD6888 in an in vitro beindin
Publikováno v:
Tetrahedron: Asymmetry. 5:723-730
Novel chiral sulfides, derived from pinene, have been prepared, converted to sulfonium salts and treated with base and aldehydes to generate non-racemic epoxides. Low to moderate enantioselectivities were obtained in the product epoxides and this pos
Autor:
Lena Scheibenflug, Johan Botling, Michael Bergqvist, Larry Mansouri, Kristina Lamberg, Fredrik Nyberg, Hanna Göransson Kultima, Mats Lambe, Simon Ekman, Lars Holmberg, Anders Berglund, Gunnar Myrdal, Andrew Peter Thomas, Patrick Micke, Anders Isaksson, Karolina Edlund, Annsofie Andersson
Publikováno v:
Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 6(11)
IntroductionNon-small cell lung cancer (NSCLC) is characterized by a multitude of genetic aberrations with unknown clinical impact. In this study, we aimed to identify gene copy number changes that correlate with clinical outcome in NSCLC. To maximiz
Publikováno v:
ChemInform. 25
Novel chiral sulfides, derived from pinene, have been prepared, converted to sulfonium salts and treated with base and aldehydes to generate non-racemic epoxides. Low to moderate enantioselectivities were obtained in the product epoxides and this pos