Browsing Closed Research Teams by author "Smith, Graham"
Now showing items 1-13 of 13
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A general [<SUP>18</SUP>F]AlF radiochemistry procedure on two automated synthesis platforms
Allott, L; Da Pieve, C; Turton, DR; Smith, G (ROYAL SOC CHEMISTRY, 2017-02-01)<p>The first general [<sup>18</sup>F]AIF automated radiolabelling procedure developed on the GE Tracerlab FX FN (Left) and Trasis AllInOne (Right) platforms.</p> -
A practical microwave method for the synthesis of fluoromethy 4-methylbenzenesulfonate in tert-amyl alcohol.
Brocklesby, KL; Waby, JS; Cawthorne, C; Smith, G (PERGAMON-ELSEVIER SCIENCE LTD, 2018-04-25)Fluorine substitution is an established tool in medicinal chemistry to favourably alter the molecular properties of a lead compound of interest. However, gaps still exist in the library of synthetic methods for accessing ... -
Affibody-Based PET Imaging to Guide EGFR-Targeted Cancer Therapy in Head and Neck Squamous Cell Cancer Models.
Burley, TA; Da Pieve, C; Martins, CD; Ciobota, DM; Allott, L; et al. (SOC NUCLEAR MEDICINE INC, 2019-03-01)In head and neck squamous cell cancer, the human epidermal growth factor receptor 1 (EGFR) is the dominant signaling molecule among all members of the family. So far, cetuximab is the only approved anti-EGFR monoclonal ... -
An alternative synthesis of Vandetanib (Caprelsa™) via a microwave accelerated Dimroth rearrangement.
Brocklesby, KL; Waby, JS; Cawthorne, C; Smith, G (PERGAMON-ELSEVIER SCIENCE LTD, 2017-04-12)Vandetanib is an orally available tyrosine kinase inhibitor used in the treatment of cancer. The current synthesis proceeds via an unstable 4-chloroquinazoline, using harsh reagents, in addition to requiring sequential ... -
Design, synthesis and in vitro characterization of fluorescent and paramagnetic CXCR4-targeted imaging agents.
Tietz, O; Kamaly, N; Smith, G; Shamsaei, E; Bhakoo, KK; et al. (2013-01-01)The G-protein coupled C-X-C chemokine receptor type 4 (CXCR4) is highly overexpressed in a range of cancers and is therefore an excellent biomarker for cancer imaging. To this end targeted iron oxide nanoparticles were ... -
Efficient [(18)F]AlF Radiolabeling of ZHER3:8698 Affibody Molecule for Imaging of HER3 Positive Tumors.
Da Pieve, C; Allott, L; Martins, CD; Vardon, A; Ciobota, DM; et al. (AMER CHEMICAL SOC, 2016-08-17)The human epidermal growth factor receptor 3 (HER3) is overexpressed in several cancers, being linked to a more resistant phenotype and hence leading to poor patient prognosis. Imaging HER3 is challenging owing to the ... -
Evaluation of DFO-HOPO as an octadentate chelator for zirconium-89.
Allott, L; Da Pieve, C; Meyers, J; Spinks, T; Ciobota, DM; et al. (ROYAL SOC CHEMISTRY, 2017-07-27)The future of 89Zr-based immuno-PET is reliant upon the development of new chelators with improved stability compared to the currently used deferoxamine (DFO). Herein, we report the evaluation of the octadentate molecule ... -
HER3-Mediated Resistance to Hsp90 Inhibition Detected in Breast Cancer Xenografts by Affibody-Based PET Imaging.
Martins, CD; Da Pieve, C; Burley, TA; Smith, R; Ciobota, DM; et al. (AMER ASSOC CANCER RESEARCH, 2018-04-15)Purpose: Recent studies have highlighted a role of HER3 in HER2-driven cancers (e.g., breast cancer), implicating the upregulation of the receptor in resistance to HER-targeted therapies and Hsp90 inhibitors (e.g., AUY922). ... -
Identification of ABC Transporter Interaction of a Novel Cyanoquinoline Radiotracer and Implications for Tumour Imaging by Positron Emission Tomography.
Slade, RL; Pisaneschi, F; Nguyen, Q-D; Smith, G; Carroll, L; et al. (PUBLIC LIBRARY SCIENCE, 2016-08-23)BACKGROUND: The epidermal growth factor receptor (EGFR) is overexpressed in many cancers including lung, ovarian, breast, head and neck and brain. Mutation of this receptor has been shown to play a crucial role in the ... -
Metal-based imaging agents: progress towards interrogating neurodegenerative disease.
Sedgwick, AC; Brewster, JT; Harvey, P; Iovan, DA; Smith, G; et al. (ROYAL SOC CHEMISTRY, 2020-05-21)Central nervous system (CNS) neurodegeneration is defined by a complex series of pathological processes that ultimately lead to death. The precise etiology of these disorders remains unknown. Recent efforts show that a ... -
Radiosynthesis of the anticancer nucleoside analogue Trifluridine using an automated 18F-trifluoromethylation procedure.
King, A; Doepner, A; Turton, D; Ciobota, DM; Da Pieve, C; et al. (ROYAL SOC CHEMISTRY, 2018-04-25)Trifluoromethyl groups are widespread in medicinal chemistry, yet there are limited 18F-radiochemistry techniques available for the production of the complementary PET agents. Herein, we report the first radiosynthesis of ... -
Synthesis and pre-clinical evaluation of a [F-18] fluoromethyl-tanaproget derivative for imaging of progesterone receptor expression
Merchant, S; Allott, L; Carroll, L; Tittrea, V; Kealey, S; et al. (ROYAL SOC CHEMISTRY, 2016-01-01)<p>This work features the synthesis and biological evaluation of a novel fluorinated derivative of tanaproget and a carbon-11 labelled analogue, a high affinity non-steroidal PR ligand, as a possible candidate for imaging ... -
Synthesis of a benzoxazinthione derivative of tanaproget and pharmacological evaluation for PET imaging of PR expression.
Allott, L; Miranda, C; Hayes, A; Raynaud, F; Cawthorne, C; et al. (SPRINGERNATURE, 2019-12-01)BACKGROUND: The histological evaluation of estrogen receptor (ER) and progesterone receptor (PR) expression in breast cancer lesions from biopsy tissue can stratify patients to receive endocrine therapy. Furthermore, PR ...