Zobrazeno 1 - 10
of 15
pro vyhledávání: '"George B. Hill"'
Autor:
Joseph B. Sweeney, George B. Hill
Publikováno v:
Journal of Chemical Education. 92:488-496
Reaction workup can be a complex problem for those facing novel synthesis of difficult compounds for the first time. Workup problem solving by systematic thinking should be inculcated as mid-graduate-level is reached. A structured approach is propose
Autor:
Clare Lane, Nicola Colclough, Les A. Dakin, M. Raymond V. Finlay, Claudio Chuaqui, Mark J. Anderton, Christopher G. Chorley, Matthew Grist, Darren Cross, Richard A. Ward, Michael J. Waring, Teresa Klinowska, Jonathon P. Orme, Cath Eberlein, Judit E. Debreczeni, Scott W. Martin, Matthew R. Box, Peter D. Smith, Susan Ashton, Paul A. Bethel, Fengjiang Wang, Sam Butterworth, George B. Hill
Publikováno v:
Journal of Medicinal Chemistry. 56:7025-7048
A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with gefitinib and erlotinib. Our reported compounds also
Autor:
Andrew A. Mortlock, George B. Hill
Publikováno v:
Synthesis. 2007:1697-1701
Two novel syntheses of a key 4-aminopyrazole synthetic building block are described. Both routes avoid the potentially explosive precursors that were used in the previously patented route. A salt of a vinamidinium cation previously used in 5-aminopyr
Valuable Synthetic Building Blocks: Useful 2-Substituted 5-Aminopyrimidines from a Stable Precursor
Publikováno v:
Synthesis. 2005:1817-1821
An efficient large-scale synthesis of 5-aminopyrimidine derivatives is described. The dihexafluorophosphate salt of a vinamidinium cation important in 5-aminopyrimidine synthesis has been prepared as a stable, easily purified intermediate. It has bee
Autor:
Peter Ballard, Michael James, Daniel S. James, Peter D. Smith, Simon J. Brown, M. Raymond V. Finlay, Michael J. Waring, Paula Perkins, Andrew D. Campbell, Heather L. McFarland, David Perkins, Gordon S. Currie, Gillian M. Lamont, Graham Richmond, Matthew R. Box, David Whittaker, Mark J. Anderton, Richard A. Ward, Teresa Klinowska, Scott G. Lamont, Nicola Colclough, Stuart L. Wells, Darren Cross, Gail L. Wrigley, George B. Hill, Nathaniel G. Martin, Paul D. Kemmitt, Susan Ashton, Lorraine A. Hassall, Paul A. Bethel, Robert Hugh Bradbury, Sam Butterworth, Christopher G. Chorley, Martine J. Mellor, Matthew Grist, Jonathon P. Orme
Publikováno v:
Journal of medicinal chemistry. 57(20)
Epidermal growth factor receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring sensitizing (or activating) mutations for a number of years. Despite encouraging clinical efficacy
Autor:
William B. Morris, George B. Hill, Neil J. Hales, C. Jane Cunliffe, Trevor J. Franklin, Andrew J. Millest, Donna Johnstone
Publikováno v:
Biochemical Society Transactions. 19:812-815
Introduction Progressive fibro-proliferative diseases (FPDs), such as liver cirrhosis, pulmonary fibrosis, scleroderma, ankylosing spondylitis and rheumatoid arthritis, exhibit excessive production of connective tissue and the resulting destruction o
Autor:
Georges Rene Pasquet, Robert W. Wilkinson, Stephen Green, Andrew A. Mortlock, Simon P. Heaton, Nicola Murdoch Heron, Sarah Kearney, Rajesh Odedra, Kevin Michael Foote, Madeleine C. Brady, Nicholas Keen, George B. Hill, Stephen R. Wedge, Frederic Henri Jung
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(6)
A new class of 1-acetanilide-4-aminopyrazole-substituted quinazoline Aurora kinase inhibitors has been discovered possessing highly potent cellular activity. Continuous infusion into athymic mice bearing SW620 tumors of the soluble phosphate derivati
Autor:
Liz Khatri, D McKillop, David Perkins, Nicola J. Roberts, Cyril B. Dousson, Elaine Brown, Stephen Green, Andrew A. Mortlock, Robert W. Wilkinson, Sarah Kearney, and Tony Parry, Rajesh Odedra, Nicolas Warin, Glenn Hatter, Nicholas Keen, Kevin Michael Foote, Trevor Johnson, Jean-Jacques Marcel Lohmann, Simon P. Heaton, Fabrice Renaud, Chris De Savi, Nicola Murdoch Heron, Frederic Henri Jung, Stephen Brightwell, Madeleine C. Brady, Georges Rene Pasquet, Steve Rhead, George B. Hill, Stephen R. Wedge, Claire Crafter, Katherine Thompson
Publikováno v:
Journal of medicinal chemistry. 50(9)
The Aurora kinases have been the subject of considerable interest as targets for the development of new anticancer agents. While evidence suggests inhibition of Aurora B kinase gives rise to the more pronounced antiproliferative phenotype, the most c
Autor:
Nicola J. Roberts, Robert W. Wilkinson, Stephen Brightwell, Hervé Germain, Cyril B. Dousson, Jean-Jacques Marcel Lohmann, Trevor Johnson, Nicola Murdoch Heron, Nicolas Warin, Rajesh Odedra, Fabrice Renaud, Chris De Savi, Andrew A. Mortlock, Elaine Brown, Christine Lambert-van der Brempt, Georges Rene Pasquet, Nicholas Keen, Katherine Thompson, George B. Hill, Stephen R. Wedge, Frederic Henri Jung, Simon P. Heaton, Stephen Green
Publikováno v:
Journal of medicinal chemistry. 49(3)
The synthesis of a novel series of quinazolines substituted at C4 by five-membered ring aminoheterocycles is reported. Their in vitro structure-activity relationships versus Aurora A and B serine-threonine kinases is discussed. Our results demonstrat
Autor:
Andrew A. Mortlock, Jonathan M. Eden, Trevor Johnson, Nicola Murdoch Heron, Siân Rowsell, Frederic Henri Jung, Nicola J. Roberts, Jason Breed, George B. Hill, Helen H.J. McMiken, Andrew Pannifer, Jennifer H. Pink, Malcolm Anderson, Richard A. Pauptit, Stephen Green, David P. Blowers
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(5)
A novel series of 5-aminopyrimidinyl quinazolines has been developed from anilino-quinazoline 1, which was identified in a high throughput screen for Aurora A. Introduction of the pyrimidine ring and optimisation of the substituents both on this ring