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George B. Hill
Researcher at AstraZeneca
Publications - 12
Citations - 1246
George B. Hill is an academic researcher from AstraZeneca. The author has contributed to research in topics: Quinazoline & Aurora B kinase. The author has an hindex of 8, co-authored 12 publications receiving 1088 citations.
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Journal ArticleDOI
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor
M. Raymond V. Finlay,Mark J. Anderton,Susan Ashton,Peter Ballard,Paul A. Bethel,Matthew R. Box,Robert Hugh Bradbury,Simon J. Brown,Sam Butterworth,Andrew D. Campbell,Christopher G. Chorley,Nicola Colclough,Darren Cross,Gordon S. Currie,Matthew Grist,Lorraine A. Hassall,George B. Hill,Daniel S. James,Michael James,Paul D. Kemmitt,Teresa Klinowska,Gillian M. Lamont,Scott G. Lamont,Nathaniel G. Martin,Heather L. McFarland,Martine J. Mellor,Jonathon P. Orme,David Perkins,Paula Perkins,Graham Richmond,Peter D. Smith,Richard A. Ward,Michael J. Waring,David Whittaker,Stuart L. Wells,Gail L. Wrigley +35 more
TL;DR: Following observations of significant tumor inhibition in preclinical models, the clinical candidate AZD9291 was administered clinically to patients with T790M positive EGFR-TKI resistant NSCLC and early efficacy has been observed, accompanied by an encouraging safety profile.
Journal ArticleDOI
Discovery, Synthesis, and in Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase
Andrew A. Mortlock,Kevin Michael Foote,Nicola Murdoch Heron,Frederic Henri Jung,Georges Rene Pasquet,Jean-Jacques Marcel Lohmann,Nicolas Warin,Fabrice Renaud,Chris De Savi,Nicola J. Roberts,Trevor Johnson,Cyril B. Dousson,George B. Hill,David Perkins,Glenn Hatter,Robert W. Wilkinson,Stephen R. Wedge,Simon P. Heaton,Rajesh Odedra,Nicholas Keen,Claire Crafter,Elaine Brown,Katherine Thompson,Stephen Brightwell,Liz Khatri,Madeleine C. Brady,Sarah Kearney,D McKillop,Steve Rhead,and Tony Parry,Stephen Green +30 more
TL;DR: A series of pyrazoloquinazolines, some of which show greater than 1000-fold selectivity for Aurora B over Aurora A kinase activity, in recombinant enzyme assays, are discovered, and compound 5 (AZD1152) has been selected for clinical evaluation and is currently in phase 1 clinical trials.
Journal ArticleDOI
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
Richard A. Ward,Mark J. Anderton,Susan Ashton,Paul A. Bethel,Matthew R. Box,Sam Butterworth,Nicola Colclough,Christopher G. Chorley,Claudio Chuaqui,Darren Cross,Les A. Dakin,Judit E. Debreczeni,Cath Eberlein,M. Raymond V. Finlay,George B. Hill,Matthew Grist,Teresa Klinowska,Clare Lane,Scott W. Martin,Jonathon P. Orme,Peter D. Smith,Fengjiang Wang,Michael J. Waring +22 more
TL;DR: A novel series of small-molecule inhibitors 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, demonstrates high levels of activity and shows selectivity over wild-type EGFR.
Journal ArticleDOI
Sar and Inhibitor Complex Structure Determination of a Novel Class of Potent and Specific Aurora Kinase Inhibitors.
Nicola Murdoch Heron,Malcolm Anderson,David P. Blowers,Jason Breed,Jonathan M. Eden,Stephen Green,George B. Hill,Trevor Johnson,Frederic Henri Jung,Helen H.J. McMiken,Andrew A. Mortlock,Andrew Pannifer,Richard A. Pauptit,Jennifer H. Pink,Nicola J. Roberts,Siân Rowsell +15 more
TL;DR: 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 showing the importance of the benzamido group in achieving selectivity.
Journal ArticleDOI
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Frederic Henri Jung,Georges Rene Pasquet,Christine Lambert-van der Brempt,Jean-Jacques Marcel Lohmann,Nicolas Warin,Fabrice Renaud,Hervé Germain,Chris De Savi,Nicola J. Roberts,Trevor Johnson,Cyril B. Dousson,George B. Hill,Andrew A. Mortlock,Nicola Murdoch Heron,Robert W. Wilkinson,Stephen R. Wedge,Simon P. Heaton,Rajesh Odedra,Nicholas Keen,Stephen Green,Elaine Brown,Katherine Thompson,Stephen Brightwell +22 more
TL;DR: The results demonstrate that quinazolines with a substituted aminothiazole at C4 possess potent Aurora A and B inhibitory activity and excellent selectivity against a panel of various serine-threonine and tyrosine kinases, as exemplified by compound 46.