C
Craig S. Donald
Researcher at AstraZeneca
Publications - 39
Citations - 1205
Craig S. Donald is an academic researcher from AstraZeneca. The author has contributed to research in topics: Stille reaction & Alkylation. The author has an hindex of 17, co-authored 39 publications receiving 1071 citations.
Papers
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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
Design of a potent, soluble glucokinase activator with excellent in vivo efficacy.
Darren Mckerrecher,Joanne V. Allen,Peter William Rodney Caulkett,Craig S. Donald,Mark L. Fenwick,Emma Grange,Keith M. Johnson,Craig Johnstone,Clifford David Jones,Kurt Gordon Pike,Rayner John Wall,Rolf Peter Walker +11 more
TL;DR: The use of unbound clearance as an optimisation parameter facilitated the identification of GKA50, a compound which combines excellent potency and pharmacokinetics with good free drug levels and solubility, and exhibits in vivo efficacy at 1mg/kg po in an acute rat OGTT model.
Patent
Carbazole derivatives and their use as neuropeptide y5 receptor ligands
TL;DR: In this paper, the authors describe the preparation and use of NPY 5 inhibitors using compounds of formula (I): R1-R6 and m are as defined within, and processes for their preparation and their use as NPY5 inhibitors are described.
Journal ArticleDOI
Discovery and Optimization of a Series of Carbazole Ureas as NPY5 Antagonists for the Treatment of Obesity
Michael Howard Block,Scott Boyer,Wayne Brailsford,David Robert Brittain,Debra Carroll,Steve Chapman,David S. Clarke,Craig S. Donald,Kevin Michael Foote,Linda Godfrey,Anthony Ladner,Marsham Pr,David J. Masters,Christine Mee,Michael R. O’Donovan,J. Elizabeth Pease,Adrian Pickup,Rayner John Wall,Andrew D. Roberts,Paul Schofield,and Abid Suleman,Andrew V. Turnbull +21 more
TL;DR: NPY5RA-972 (4o) is a highly potent Y5 antagonist in vivo but does not block neuropeptide Y-induced feeding nor does it reduce feeding in rats, suggesting that the Y5 receptor alone has no significant role in feeding in these models.