Nigel A. Lengkeek

ORCID: 0000-0003-0612-8024
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About
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Research Areas
  • Crystallization and Solubility Studies
  • X-ray Diffraction in Crystallography
  • Radiopharmaceutical Chemistry and Applications
  • Medical Imaging Techniques and Applications
  • Lanthanide and Transition Metal Complexes
  • Cancer, Hypoxia, and Metabolism
  • Supramolecular Chemistry and Complexes
  • Metal complexes synthesis and properties
  • Crystallography and molecular interactions
  • Molecular Sensors and Ion Detection
  • Magnetism in coordination complexes
  • Nanoplatforms for cancer theranostics
  • Medical Imaging and Pathology Studies
  • Organometallic Complex Synthesis and Catalysis
  • Luminescence and Fluorescent Materials
  • Porphyrin and Phthalocyanine Chemistry
  • Nanoparticle-Based Drug Delivery
  • Radioactive element chemistry and processing
  • Click Chemistry and Applications
  • Chemical Synthesis and Analysis
  • Cancer-related Molecular Pathways
  • Synthesis of Tetrazole Derivatives
  • Photochromic and Fluorescence Chemistry
  • Metal-Catalyzed Oxygenation Mechanisms
  • Enzyme function and inhibition

The University of Western Australia
2008-2023

Australian Nuclear Science and Technology Organisation
2012-2022

Australian National University
2008

Université de Strasbourg
2004

Large metal-oxo clusters consistently assume spherical or regular polyhedral morphologies rather than high-aspect-ratio structures. Access to elongated core structures has now been achieved by the reaction of lanthanoid salts with a tetrazole-functionalized calixarene in presence simple carboxylate co-ligand. The resulting Ln19 and Ln12 are constructed from apex-fused Ln5O6 trigonal bipyramids formed under range conditions reagent ratios. Altering co-ligand structure reliably controls...

10.1021/ja506677h article EN publisher-specific-oa Journal of the American Chemical Society 2014-10-04

Our aim was to report the use of <sup>64</sup>Cu and <sup>67</sup>Cu as a theranostic pair radionuclides in human subjects. An additional measure whole-organ dosimetry attached somatostatin analog octreotate using sarcophagine MeCOSar chelator (SARTATE) subjects with receptor–expressing lesions confined cranium, thereby permitting normal-organ for remainder body. <b>Methods:</b> Pretreatment PET imaging studies were performed up 24 h after injection [<sup>64</sup>Cu]Cu-SARTATE, estimated...

10.2967/jnumed.122.264586 article EN Journal of Nuclear Medicine 2022-12-02

Tumor hypoxia contributes resistance to chemo- and radiotherapy, while oxygenated tumors are sensitive these treatments. The indirect detection of hypoxic is possible by targeting carbonic anhydrase IX (CA IX), an enzyme overexpressed in tumors, with sulfonamide-based imaging agents. In this study, we present the design synthesis novel gallium-radiolabeled small-molecule sulfonamides CA IX. compounds display favorable vivo pharmacokinetics stability. We demonstrate that our lead compound,...

10.1021/acs.jmedchem.6b00623 article EN Journal of Medicinal Chemistry 2016-06-20

Abstract: Physiologically stable multimodality imaging probes for positron emission tomography/single-photon computed tomography (PET/SPECT)-magnetic resonance (MRI) were synthesized using the superparamagnetic maghemite iron oxide (γ-Fe 2 O 3 ) nanoparticles (SPIONs). The SPIONs sterically stabilized with a finely tuned mixture of diblock copolymers either methoxypolyethylene glycol (MPEG) or primary amine NH end groups. radioisotope PET SPECT was incorporated at high temperature. 57 Co 2+...

10.2147/ijn.s127171 article EN cc-by-nc International Journal of Nanomedicine 2017-01-01

Given the strong clinical evidence that copper levels are significantly elevated in a wide spectrum of tumors, homeostasis is considered as an emerging target for anticancer drug design.Monitoring vivo therefore paramount importance when assessing efficacy copper-targeting drugs.Herein, we investigated activity compound Dextran-Catechin by developing [ 64 Cu]CuCl2 PET imaging protocol to monitor its effect on tumors.Methods: Protein expression transporter 1 (CTR1) tissue microarrays...

10.7150/thno.29840 article EN cc-by Theranostics 2018-01-01

Structural studies of seven very differently functionalised derivatives calix[4]arene have been used to provide an analysis the numerous factors which may influence solvent adduct formation by calixarenes. Evidence is presented that even where a guest included within calixarene cavity, interactions solely cavity cannot be seen as sole influences upon position and orientation.

10.1039/b308214h article EN Organic & Biomolecular Chemistry 2004-01-01

Abstract Herein we describe the preparation and structure‐activity relationship studies on range of stilbene based compounds their antibacterial activity. Two related compounds, each bearing carboxylic acid moieties, exhibit good activity against several bacterial strains, including methicillin‐resistant Staphylococcus aureus MRSA (ATCC 33592 NCTC 10442). Compound 10 was most active Moraxella catarrhalis with minimum inhibitory concentrations (MICs) 0.12–0.25 μg mL −1 spp. MICs ranging from...

10.1002/chem.201303119 article EN Chemistry - A European Journal 2013-11-18

A series of complexes with π-conjugated carbon chains terminated by bipyridyl moieties has been prepared. These allenylidene were derived from 9-hydroxy-9-ethynyl-4,5-diazafluorene, the preparation which is reported; new are highly colored cumulated chain terminating in a unit providing site for further coordination. The synthesis, characterization, and X-ray structure determination trans-[MCl(P∩P)2═C═C═(4,5-diazafluoren-9-yl)]PF6 (M = Ru, P∩P bis(diphenylphosphino)methane (dppm),...

10.1021/om700824g article EN Organometallics 2008-03-19

Dedication: One of Alan Sargeson’s great abilities was to seek out knowledge on topics which he not the master from those people with expertise. This led occasionally publications a ‘cricket team’ authors but rich brew information, often international. also insisted that all were equal since, without any one, paper would be what it was. Hence, endeavoured pursue policy, difficult maintain over period where an obsession absurdities such as order and point-scoring based meaningless publication...

10.1071/ch09356 article EN Australian Journal of Chemistry 2009-01-01

Thirteen compounds in a new class of fluorinated 5-pyrrolidinylsulfonyl isatin derivatives were synthesised that have potent and selective inhibitory activity against effector caspases-3 -7. With vivo animal PET imaging studies cerebral ischemia being planned, N-benzylation with selected para-substituted benzylic halides allowed systematic variation lipophilicity (logP 1.94–3.31) without decreasing inhibition potency (IC50). From this series the p-methoxybenzyl analogue was for initial...

10.1039/c2md20249b article EN MedChemComm 2012-11-12

A highly efficient synthesis of p-carboethoxy-tristyryl and carboethoxy-terastyrenyl benzene derivatives through a multiple Heck cross coupling reaction is reported. This provides an route to DNA intercalator precursors containing core.

10.1071/ch10374 article EN Australian Journal of Chemistry 2011-01-01

DOTA-linked glutamine analogues with a C6- alkyl and polyethyleneglycol (PEG) chain between the chelating group L-glutamine moiety were synthesised labelled 67,68Ga using established methods. High yields achieved for radiolabelling of molecules both radionuclides (&gt;90%), although conversion commercially available 67Ga-citrate to chloride species was requirement consistent high radiochemical yields. The generator produced 68Ga in [68Ga(OH)4]− form. 67Ga complexes demonstrated be stable PBS...

10.3390/molecules18067160 article EN cc-by Molecules 2013-06-19

This study reports the synthesis, [123I]radiolabeling, and biological profile of a new series iodinated compounds for potential translation to corresponding [131I]radiolabeled radionuclide therapy melanoma. Radiolabeling was achieved via standard electrophilic iododestannylation in 60–90% radiochemical yield. Preliminary SPECT imaging demonstrated high distinct tumor uptake all compounds, as well tumor-to-background ratios compared literature compound [123I]4 (ICF01012). The most favorable...

10.1021/acs.jmedchem.5b00777 article EN Journal of Medicinal Chemistry 2015-07-15

A domino Horner−Wadsworth−Emmons olefination strategy has been used to prepare homologous series of (polyen)ones, and through combinatorial elaboration, corresponding families highly branched hydrocarbons. Gas chromatography−mass spectrometry the mixtures enabled rapid unambiguous identification several alkanes geochemical importance. This is first example use synthesis for elucidation structural connectivity.

10.1021/cc900134t article EN Journal of Combinatorial Chemistry 2009-12-14

The synthesis and characterisation of p-t-butylcalix[4]arene functionalised at the lower rim with four tetrazole moieties is reported. macrocycle found to be a poorer ionophore for lanthanoid cations than bis-tetrazole–substituted analogue. Solution-phase photophysical studies strongly suggested that interacted only weakly calixarene ligand. A mixed sodium/triethylammonium salt ligand was crystallised in presence structurally characterised. Strong intramolecular interactions are hypothesised...

10.1080/10610278.2015.1075536 article EN Supramolecular chemistry 2015-10-23

Various 2- and 3-thienylmethylamino-substituted cobalt(III) cage amine complexes, prepared with the objective of obtaining cage-functionalized polythienyls, have been found to be resistant oxidative polymerization by both electrochemical chemical procedures. X-ray structure determinations indicate that there is negligible perturbation physical dimensions thiophene moieties substituents thus resistance must associated high positive charge carried these substituents.

10.1021/ic9019603 article EN Inorganic Chemistry 2010-03-03

Delocalized lipophilic cations such as tri- and tetra-arylphosphonium are able to diffuse across the mitochondrial membrane, which allows them selectively accumulate in cells with a high transmembrane potential (ΔΨm ). The membrane of cancer cardiomyocytes has been reported be significantly higher than that normal epithelial cells. This feature can exploited for selective accumulation phosphonium derivatives purposes molecular imaging using radionuclides. Four structurally related...

10.1002/jlcr.3448 article EN Journal of Labelled Compounds and Radiopharmaceuticals 2016-11-07

Abstract To improve the signal‐to‐noise ratio of hypoxia positron emission tomography (PET) imaging, stimuli‐responsive polymers are designed for delivery PET tracer fluorine‐18 labeled fluoromisonidazole ([ 18 F]FMISO). Linear poly( N ‐(2‐(hydroxypropyl)methacrylamide)) functionalized with hydrazide linkers that form pH‐sensitive acyl hydrazone bonds after their conjugation to an [ F]FMISO ketone analogue. The release analogue from is considerably faster at a lower pH and its uptake...

10.1002/marc.202000061 article EN Macromolecular Rapid Communications 2020-04-06

A limitation to the wider introduction of personalised dosimetry in theranostics is relative paucity imaging radionuclides with suitable physical and chemical properties be paired a long-lived therapeutic partner. As most beta-emitting emit gamma radiation as well they could potentially used radionuclide radionuclide. However, downsides are that beta will deliver significant dose part treatment planning procedure, branching ratio often quite low. Gallium-67 has been use nuclear medicine for...

10.22038/aojnmb.2020.51714.1355 article EN DOAJ (DOAJ: Directory of Open Access Journals) 2021-01-01
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