S
Sarah A. Loddick
Researcher at AstraZeneca
Publications - 7
Citations - 246
Sarah A. Loddick is an academic researcher from AstraZeneca. The author has contributed to research in topics: Prostate cancer & Androgen receptor. The author has an hindex of 6, co-authored 7 publications receiving 221 citations.
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Journal ArticleDOI
AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function In Vitro and In Vivo
Sarah A. Loddick,Sarah Ross,Andrew G. Thomason,David Robinson,Graeme Walker,Tom Dunkley,Sandra R. Brave,Nicola Broadbent,Natalie Stratton,Dawn Trueman,Elizabeth Mouchet,Fadhel Shaheen,Vivien Jacobs,Marie Cumberbatch,Joanne Wilson,Rhys D.O. Jones,Robert Hugh Bradbury,Alfred A. Rabow,Luke Gaughan,Chris Womack,Simon T. Barry,Craig N. Robson,Susan E. Critchlow,Stephen R. Wedge,A. Nigel Brooks +24 more
TL;DR: The biological characterization of AZD3514 is described, an orally bioavailable drug that inhibits androgen-dependent and -independent AR signaling and shows antitumor activity in the HID28 mouse model of CRPC in vivo.
Journal ArticleDOI
The Discovery of Azd5597, a Potent Imidazole Pyrimidine Amide Cdk Inhibitor Suitable for Intravenous Dosing.
Clifford David Jones,David M. Andrews,Barker Andrew John,Kevin Blades,Paula Daunt,S J East,Catherine Geh,Mark A. Graham,Keith M. Johnson,Sarah A. Loddick,Heather M. McFarland,Alexandra McGregor,Louise Moss,David Alan Rudge,Peter B. Simpson,Swain Michael Lingard,Kin Yip Tam,Julie A. Tucker,Michael A. Walker +18 more
TL;DR: Optimisation of inhibitory potency against multiple CDK's resulted in imidazole pyrimidine amides with potent in vitro anti-proliferative effects against a range of cancer cell lines.
Journal ArticleDOI
Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer.
Robert Hugh Bradbury,Neil James Hales,Alfred A. Rabow,Graeme Walker,David G. Acton,David M. Andrews,Peter Ballard,Nigel Brooks,Nicola Colclough,Alan Girdwood,Urs Hancox,Owen Jones,David A. Jude,Sarah A. Loddick,Andrew A. Mortlock +14 more
TL;DR: A medicinal chemistry program derived from a novel androgen receptor ligand 8a led to 6-[4-cyanobenzyl)piperazin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazine (10b), for which high plasma levels following oral administration in a preclinical model compensate for moderate cellular potency.
Journal ArticleDOI
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer
Robert Hugh Bradbury,David G. Acton,Nicola Broadbent,A. Nigel Brooks,Carr Gregory Richard,Glenn Hatter,Barry R. Hayter,Hill Kathryn Jane,Nicholas J. Howe,Rhys D.O. Jones,David A. Jude,Scott G. Lamont,Sarah A. Loddick,Heather L. McFarland,Zaieda Parveen,Alfred A. Rabow,Gorkhn Sharma-Singh,Natalie Stratton,Andrew G. Thomason,Dawn Trueman,Graeme Walker,Stuart L. Wells,Joanne Wilson,J. Matthew Wood +23 more
TL;DR: Clinical candidate 6-(4-{4-[2-acetylpiperazin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine (12), designated AZD3514, that is being evaluated in a Phase I clinical trial in patients with castrate-resistant prostate cancer.
Journal ArticleDOI
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode
M. Raymond V. Finlay,David G. Acton,David M. Andrews,Barker Andrew John,Michael Dennis,Eric Fisher,Mark A. Graham,Clive Green,David William AstraZeneca R D Alderley Heaton,Galith Karoutchi,Sarah A. Loddick,Rémy Morgentin,Andrew D. Roberts,Julie A. Tucker,Hazel M. Weir +14 more
TL;DR: A piperazine series of cyclin-dependent kinase (CDK) inhibitors have been identified that exhibit excellent physiochemical properties and a novel binding mode, whereby a bridging interaction via a water molecule with Asp 86 of CDK2, leads to selectivity for the CDK family of enzymes over other kinases.