A Synthetic Overview of Radiolabeled Compounds for β‐Amyloid Targeting

Morais, Goreti Ribeiro; Paulo, António; Santos, Isabel

doi:10.1002/ejoc.201101449

Cited by 16 publications

(3 citation statements)

References 114 publications

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“…In Alzheimer’s, for example, A-β peptides form fibrillar deposits in amyloid plaques that invade the brain’s regions of memory and cognition, before spreading to other areas. Important advances have already been made in PET imaging of A-β lesions, but progress is much more mitigated in the case of SPECT imaging, particularly using 99m Tc complexes . Pirmettis et al described fluorescent [2 + 1] Re(I) tricarbonyl complexes with a curcumin derivative acting as a bidentate (O,O) ligand and with imidazole or isocyanocyclohexane as unidentate coligands.…”

Section: Target-specific Complexesmentioning

confidence: 99%

Organometallic Complexes for SPECT Imaging and/or Radionuclide Therapy

Morais¹,

Paulo²,

Santos³

2012

Organometallics

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This article reviews Re and Tc organometallic chemistry and radiochemistry, focusing on the most relevant aspects to design radiotools for molecular imaging and therapy. The review comprises an overview of organometallic Re and Tc complexes with relevance to the field, particularly M(I) tricarbonyl complexes stabilized by a huge variety of ligands. These include Werner type chelators, cyclopentadienyls, carboranes, and poly(mercaptoazolyl)borates, which permitted the hitherto unprecedented use of M–C and M–H bonds. The most relevant biomolecules labeled with the different organometallic cores will also be reviewed, as well as the opportunities offered by the tricarbonyl approach to design high-performance perfusion agents.

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Section: Target-specific Complexesmentioning

confidence: 99%

Organometallic Complexes for SPECT Imaging and/or Radionuclide Therapy

Morais¹,

Paulo²,

Santos³

2012

Organometallics

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“…The design and radiochemistry of these selected agents will be discussed as well as the current regulatory status of the selected agents. There have been several reviews of a wider scope published and readers are directed to these for additional information regarding in vitro applications and the design of radiolabeled and/or fluorescent probes for use in in vitro or in vivo imaging of A β plaques . The PET imaging agents included in this review comprise three broad structural classes: naphthalene analogs, planar heteroaromatic compounds (benzothiazoles, benzoxazole analogs, and benzofurans), and diaryl alkene analogs.…”

Section: Introductionmentioning

confidence: 99%

Positron emission tomography radioligands for in vivo imaging of Aβ plaques

Mason

Mathis²,

Klunk

2013

Labelled Comp Radiopharmac

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The development of positron emission tomography (PET) radioligands for the non-invasive imaging of amyloid-β plaque burden has been the focus of intense research efforts over the last decade. A variety of structural backbones have been investigated and several radiolabeled molecules have been evaluated in phase I (and later) clinical studies. These efforts have been driven by the desire not only to develop a suitable diagnostic imaging agent but also to develop a means to evaluate potential therapies for Alzheimer’s disease. This review focuses on the development of these ligands, as well as the radiochemistry and current regulatory status of these PET radioligands. Particular attention is given to those ligands that have progressed to the later stages of drug development (phase II/III clinical trial studies) or approved New Drug Application status.

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“…The development of probes for amyloid plaques and tangles 17,18 provides one avenue for the noninvasive diagnosis and evaluation of AD progression in living subjects and its differentiation from age-related cognitive decline in AD patients. 19,20 We report the synthesis of a radiolabeled Congo Red analog, ( E,E )-1-[ 3 H]-2,5-bis(4’-hydroxy-3’-carboxystyryl)benzene ( 1a ), which has not been reported previously, and its non-radiolabeled counterpart 21 1b , which is commonly known as X-34 (Fig.…”

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confidence: 99%

Tritium-labeled (E,E)-2,5-bis(4′-hydroxy-3′-carboxystyryl)benzene as a probe for β-amyloid fibrils

Матвеев

Kwiatkowski

Sviripa

et al. 2014

Bioorganic & Medicinal Chemistry Letters

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Accumulation of Aβ in the brains of Alzheimer disease (AD) patients reflects an imbalance between Aβ production and clearance from their brains. Alternative cleavage of amyloid precursor protein (APP) by processing proteases generates soluble APP fragments including the neurotoxic amyloid Aβ40 and Aβ42 peptides that assemble into fibrils and form plaques. Plaque-buildup occurs over an extended time-frame, and the early detection and modulation of plaque formation are areas of active research. Radiolabeled probes for the detection of amyloid plaques and fibrils in living subjects are important for noninvasive evaluation of AD diagnosis, progression, and differentiation of AD from other neurodegenerative diseases and age-related cognitive decline. Tritium-labeled (E,E)-1-[3H]-2,5-bis(4’-hydroxy-3’-carbomethoxystyryl)benzene possesses an improved level of chemical stability relative to a previously reported radioiodinated analog for radiometric quantification of Aβ plaque and tau pathology in brain tissue and in vitro studies with synthetic Aβ and tau fibrils.

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A Synthetic Overview of Radiolabeled Compounds for β‐Amyloid Targeting

Cited by 16 publications

References 114 publications

Organometallic Complexes for SPECT Imaging and/or Radionuclide Therapy

Organometallic Complexes for SPECT Imaging and/or Radionuclide Therapy

Positron emission tomography radioligands for in vivo imaging of Aβ plaques

Tritium-labeled (E,E)-2,5-bis(4′-hydroxy-3′-carboxystyryl)benzene as a probe for β-amyloid fibrils

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