L
Lorraine A. Hassall
Researcher at AstraZeneca
Publications - 22
Citations - 1038
Lorraine A. Hassall is an academic researcher from AstraZeneca. The author has contributed to research in topics: Deprotonation & Integrin. The author has an hindex of 11, co-authored 22 publications receiving 826 citations. Previous affiliations of Lorraine A. Hassall include Queen Mary University of London.
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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 of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): A Potent and Selective Inhibitor of ATR Protein Kinase with Monotherapy in Vivo Antitumor Activity
Kevin Michael Foote,Kevin Blades,Anna Cronin,Shaun M. Fillery,Sylvie S. Guichard,Lorraine A. Hassall,Ian Hickson,Xavier Jacq,Philip J. Jewsbury,Thomas M. McGuire,J. Willem M. Nissink,Rajesh Odedra,Ken Page,Paula Perkins,Abid Suleman,Kin Yip Tam,Pia Thommes,Rebecca Broadhurst,Christine M. Wood +18 more
TL;DR: The discovery and synthesis of a series of sulfonylmorpholinopyrimidines that show potent and selective ATR inhibition are described that leads to compound 6 (AZ20) which inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC50 of 5 nM.
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The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one)
Kurt Gordon Pike,Barlaam Bernard Christophe,Elaine Cadogan,Andrew D. Campbell,Yingxue Chen,Nicola Colclough,Nichola L. Davies,Camila de-Almeida,Sébastien L. Degorce,Myriam Didelot,Allan Dishington,Richard Ducray,Stephen T. Durant,Lorraine A. Hassall,Jane L. Holmes,Gareth Hughes,Philip A. MacFaul,Keith R. Mulholland,Thomas M. McGuire,Gilles Ouvry,Martin Pass,Graeme R. Robb,Natalie Stratton,Zhenhua Wang,Joanne Wilson,Baochang Zhai,Kang Zhao,Nidal Al-Huniti +27 more
TL;DR: The discovery is made of 64 (AZD0156), an exceptionally potent and selective inhibitor of ATM based on an imidazo[4,5- c]quinolin-2-one core that has good preclinical phamacokinetics, a low predicted clinical dose, and a high maximum absorbable dose.
Journal ArticleDOI
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Sébastien L. Degorce,Barlaam Bernard Christophe,Elaine Cadogan,Allan Dishington,Richard Ducray,Steven C. Glossop,Lorraine A. Hassall,Franck Lach,Alan Lau,Thomas M. McGuire,Thorsten Nowak,Gilles Ouvry,Kurt Gordon Pike,Andrew G. Thomason +13 more
TL;DR: A novel series of 3-quinoline carboxamides discovered and optimized as selective inhibitors of the ataxia telangiectasia mutated (ATM) kinase constitute excellent oral tools to probe ATM inhibition in vivo with overall ADME properties suitable for oral administration.
Journal ArticleDOI
On the choice of Lewis acids for the Prins reaction; two total syntheses of (±)-Civet
Freda K. I. Chio,Julie Warne,Damien Gough,Mark J. Penny,Sasa Green,Simon J. Coles,Michael B. Hursthouse,Peter Jones,Lorraine A. Hassall,Thomas M. McGuire,Adrian P. Dobbs +10 more
TL;DR: In this paper, the effect of the choice of Lewis acid on the outcome of the reaction and the product(s) has been investigated, yielding hitherto unseen dihydropyran products in the Prins cyclisation reaction of homoallylic alcohols.