A nuclear chocolate box: the periodic table of nuclear medicine

Blower, Philip J.

doi:10.1039/c4dt02846e

Cited by 127 publications

(116 citation statements)

References 170 publications

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“…Bis(thiosemicarbazone) ligands and their metallic complexes have been extensively investigated over the last 50 years, due to their pharmacological activity and potential in cancer 68 Ga acetate only 60 min post injection; [113] B) images of 64 Cu acetate, 64 CuATSM, and 64 CuGTSM 30 min post-injection. It can be seen how copper acetate shows a similar biodistribution to CuATSM with rapid liver uptake.…”

Section: Resultsmentioning

confidence: 99%

Applications of “Hot” and “Cold” Bis(thiosemicarbazonato) Metal Complexes in Multimodal Imaging

Cortezon‐Tamarit

Sarpaki

Calatayud

et al. 2016

The Chemical Record

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The applications of coordination chemistry to molecular imaging has become a matter of intense research over the past 10 years. In particular, the applications of bis(thiosemicarbazonato) metal complexes in molecular imaging have mainly been focused on compounds with aliphatic backbones due to the in vivo imaging success of hypoxic tumors with PET (positron emission tomography) using (64) CuATSM [copper (diacetyl-bis(N4-methylthiosemicarbazone))]. This compound entered clinical trials in the US and the UK during the first decade of the 21(st) century for imaging hypoxia in head and neck tumors. The replacement of the ligand backbone to aromatic groups, coupled with the exocyclic N's functionalization during the synthesis of bis(thiosemicarbazones) opens the possibility to use the corresponding metal complexes as multimodal imaging agents of use, both in vitro for optical detection, and in vivo when radiolabeled with several different metallic species. The greater kinetic stability of acenaphthenequinone bis(thiosemicarbazonato) metal complexes, with respect to that of the corresponding aliphatic ATSM complexes, allows the stabilization of a number of imaging probes, with special interest in "cold" and "hot" Cu(II) and Ga(III) derivatives for PET applications and (111) In(III) derivatives for SPECT (single-photon emission computed tomography) applications, whilst Zn(II) derivatives display optical imaging properties in cells, with enhanced fluorescence emission and lifetime with respect to the free ligands. Preliminary studies have shown that gallium-based acenaphthenequinone bis(thiosemicarbazonato) complexes are also hypoxia selective in vitro, thus increasing the interest in them as new generation imaging agents for in vitro and in vivo applications.

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Section: Resultsmentioning

confidence: 99%

Applications of “Hot” and “Cold” Bis(thiosemicarbazonato) Metal Complexes in Multimodal Imaging

Cortezon‐Tamarit

Sarpaki

Calatayud

et al. 2016

The Chemical Record

View full text Add to dashboard Cite

show abstract

“…Radiolabelling procedures for biomolecules still involve multiple manipulations and poor specifi c activity. Hydrazinonicotinamide (hynic) and tricarbonyl (Tc(CO) 3 + ) complexes come closest to achieving this, but both fall short and neither has led to commercial products. Due to a shift in commercial interests towards PET, very little effort has been devoted to this problem in the last decade and it remains a challenge to achieve "one-step" 99m Tc biomolecule labelling.…”

Section: J Blowermentioning

confidence: 99%

“…They were easily synthesised in hospitals using simple kit vials, fi rmly establishing 99m Tc as the staple medical radionuclide. They were largely serendipitous, arising from biological experiments using "off the shelf" chelating ligands selected without detailed knowledge of basic technetium chemistry [ 3 ], which was almost unstudied at that time. The simple preparation disguised extremely complex coordination chemistry.…”

Section: J Blowermentioning

confidence: 99%

“…This set the stage for radiotracer design to shift towards targeting specifi c receptors and transporters, by incorporating 99m Tc into peptides and proteins [ 3 ], and the term "molecular imaging" became both fashionable and relevant. It remained an important aspiration to synthesise 99m Tc-radiopharmaceuticals via simple processes that are quick and use mild, aqueous conditions, avoiding the need for purifi cation which adds undesirable complexity.…”

Section: J Blowermentioning

confidence: 99%

“…The concept of technetium "cores" emerged -well-defi ned, stable complexes adapted to the coordination preferences of technetium, that could be functionalised for different purposes. Examples include the TcO 3+ core (the basis of tracers such as MAG3 complex for renal function imaging, "pentavalent" DMSA complex for medullary thyroid carcinoma and bone disease, HMPAO complex for cerebral perfusion imaging and cell labelling), Tc(isonitrile) 6 + (sestamibi for myocardial perfusion imaging), TcO 2 + (with tetraamine or diphosphine chelating ligands such as tetrofosmin), Tc(CO) 3 + and TcN(dithiocarbamate) 2 .…”

Section: J Blowermentioning

confidence: 99%

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