Spirocyclic hypervalent iodine(III)-mediated radiofluorination of non-activated and hindered aromatics
- Benjamin H. Rotstein, Nickeisha A. Stephenson, N. Vasdev, Steven H. Liang
- Chemistry, BiologyNature Communications
- 1 May 2014
An effective solution that relies on the chemistry of spirocyclic hypervalent iodine(III) complexes, which serve as precursors for rapid, one-step regioselective radiofluorination with [18F]fluoride, allowing direct 18F labelling of highly functionalized non-activated arenes and PET radiopharmaceuticals is described.
Recent developments on PET radiotracers for TSPO and their applications in neuroimaging
- Lingling Zhang, Kuan Hu, Steven H. Liang
- BiologyActa Pharmaceutica Sinica B
- 25 August 2020
Sulfur Containing Scaffolds in Drugs: Synthesis and Application in Medicinal Chemistry.
- M. Feng, Bingqing Tang, Steven H. Liang, Xuefeng Jiang
- ChemistryCurrent Topics in Medicinal Chemistry
- 1 May 2016
Sulfonamides, thioethers, sulfones and Penicillin are the most common scaffolds in sulfur containing drugs, which are well studied both on synthesis and application during the past decades.
Mechanistic studies and radiofluorination of structurally diverse pharmaceuticals with spirocyclic iodonium(iii) ylides
- Benjamin H. Rotstein, Lu Wang, Steven H. Liang
- ChemistryChemical Science
- 24 March 2016
Theoretical studies provide insight into radiofluorination of non-activated electron-rich and sterically hindered 18F-arenes using a new class of adamantyl-based spirocyclic iodonium(iii) ylide…
Novel Fluorinated 8-Hydroxyquinoline Based Metal Ionophores for Exploring the Metal Hypothesis of Alzheimer's Disease.
- Steven H. Liang, A. Southon, N. Vasdev
- Chemistry, BiologyACS Medicinal Chemistry Letters
- 14 August 2015
In the search of metal ionophores, several promising chemical entities by strategic fluorination of 8-hydroxyquinoline drugs, clioquinol, and PBT2 are identified and suitable for further development as drug candidates and/or positron emission tomography (PET) biomarkers if radiolabeled with (18)F.
Synthesis and preliminary PET imaging of 11C and 18F isotopologues of the ROS1/ALK inhibitor lorlatinib
- T. Collier, M. Normandin, N. Vasdev
- BiologyNature Communications
- 8 June 2017
Synthetic routes to 11C- and 18F-labelled lorlatinib are developed, with subsequent PET imaging showing good blood brain barrier permeability in non-human primates, confirming that this radiotracer has high brain permeability.
11CO2 fixation: a renaissance in PET radiochemistry.
- Benjamin H. Rotstein, Steven H. Liang, N. Vasdev
- Chemistry, BiologyChemical Communications
- 28 May 2013
This review summarizes classical [( 11)C]CO2 fixation strategies using organometallic reagents and then focuses on newly developed methods that employ strong organic bases to reversibly capture [(11)C].CO2 into solution, thereby enabling highly functionalized labelled compounds to be prepared.
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.
- Steven H. Liang, J. Chen, N. Vasdev
- Biology, ChemistryAngewandte Chemie
- 8 August 2016
Preliminary PET imaging studies in non-human primates confirmed that the two major obstacles for imaging GSK-3, namely, reasonable brain permeability and displaceable binding, are overcome.
Marriage of black phosphorus and Cu2+ as effective photothermal agents for PET-guided combination cancer therapy
- Kuan Hu, Lin Xie, Ming-Rong Zhang
- EngineeringNature Communications
- 8 June 2020
It is reported that the inherent Cu2+-capturing ability of black phosphorus (BP) can accelerate the degradation of BP, while also enhancing photothermal stability, and apply this material for PET-guided, CDT-enhanced combination cancer therapy in mice.
Chemistry for Positron Emission Tomography: Recent Advances in 11 C-, 18 F-, 13 N-, and 15 O-Labeling Reactions.
- Xiaoyun Deng, Jian Rong, Steven H. Liang
- Chemistry, BiologyAngewandte Chemie
- 25 February 2019
An overview of commonly used labeling reactions through examples of clinically relevant PET tracers is provided and the most recent developments and breakthroughs over the past decade are highlighted, with a focus on 11 C, 18 F, 13 N, and 15 O.