L
Lyman Feron
Researcher at AstraZeneca
Publications - 13
Citations - 702
Lyman Feron is an academic researcher from AstraZeneca. The author has contributed to research in topics: Chemistry & Catalysis. The author has an hindex of 9, co-authored 9 publications receiving 513 citations.
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Journal ArticleDOI
AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models
Hazel M. Weir,Robert Hugh Bradbury,Mandy Lawson,Alfred A. Rabow,David Buttar,Rowena Callis,Jon Curwen,Camila de Almeida,Peter Ballard,Micheal Hulse,Craig S. Donald,Lyman Feron,Galith Karoutchi,Philip A. MacFaul,Thomas A. Moss,Richard A. Norman,Stuart E. Pearson,Michael Tonge,Gareth M. Davies,Graeme Walker,Zena Wilson,Rachel Rowlinson,Steve Powell,Claire Sadler,Graham Richmond,Brendon Ladd,Ermira Pazolli,Anne Marie Mazzola,Celina M. D'Cruz,Chris De Savi +29 more
TL;DR: The pharmacologic evidence showed that AZD9496 is an oral, nonsteroidal, selective estrogen receptor antagonist and downregulator in ER(+ breast cells that could provide meaningful benefit to ER(+) breast cancer patients.
Journal ArticleDOI
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-Fluoro-2-Methylpropyl)-3-Methyl-2, 3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indol-1-Yl)Phenyl)Acrylic Acid (Azd9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
Chris De Savi,Robert Hugh Bradbury,Alfred A. Rabow,Richard A. Norman,Camila de Almeida,David M. Andrews,Peter Ballard,David Buttar,Rowena Callis,Gordon S. Currie,Jon Curwen,Christopher D. Davies,Craig S. Donald,Lyman Feron,H. Gingell,Steven C. Glossop,Barry R. Hayter,Syeed Hussain,Galith Karoutchi,Scott G. Lamont,Philip A. MacFaul,Thomas A. Moss,Stuart E. Pearson,Michael Tonge,Graeme Walker,Hazel M. Weir,Zena Wilson +26 more
TL;DR: The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described.
Journal ArticleDOI
Branch-Selective and Enantioselective Iridium-Catalyzed Alkene Hydroarylation via Anilide-Directed C–H Oxidative Addition
TL;DR: Tertiary benzylic stereocenters are accessed in high enantioselectivity by Ir-catalyzed branch selective addition of anilide ortho-C-H bonds across styrenes and α-olefins.
Journal ArticleDOI
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2
Richard A. Ward,Nicola Colclough,Mairi Challinor,Judit E. Debreczeni,Kay Eckersley,Gary Fairley,Lyman Feron,Vikki Flemington,Mark A. Graham,Ryan Greenwood,Philip Hopcroft,Tina Howard,Michael James,Clifford David Jones,Christopher R. Jones,Jonathan Renshaw,Karen Roberts,Lindsay Snow,Michael Tonge,Kay Yeung +19 more
TL;DR: Multiple series of highly selective covalent ERK1/2 inhibitors informed by structure-based drug design (SBDD) are identified for potential in vitro and in vivo studies to assess the risks and or benefits of targeting this pathway through such a mechanism of action.
Journal ArticleDOI
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Robert Hugh Bradbury,Rowena Callis,Carr Gregory Richard,Huawei Chen,Edwin Clark,Lyman Feron,Steve C. Glossop,Mark A. Graham,Maureen Hattersley,Christopher R. Jones,Scott G. Lamont,Gilles Ouvry,Anil Patel,Joe Patel,Alfred A. Rabow,Craig A. Roberts,Stephen Stokes,Natalie Stratton,Graeme Walker,Lara Ward,David Whalley,David Whittaker,Gail L. Wrigley,Michael J. Waring,Michael J. Waring +24 more
TL;DR: The optimized compound from this campaign exhibited excellent pharmacokinetic profile and exhibited high potency in vitro and in vivo effecting c-Myc downregulation and tumor growth inhibition in xenograft studies.