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Palladium-Catalyzed Tandem Reactions via Allene Intermediates for the Rapid Synthesis of a Fused Indenone-Indole Scaffold.
Org Lett
January 2025
State Key Laboratory of Materials-Oriented Chemical Engineering, College of Chemical Engineering, Nanjing Tech University, Nanjing 211800, China.
A palladium-catalyzed tandem reaction of 1-(2-iodophenyl)-3-arylprop-2-yn-1-ones and 1-(2-azidophenyl)propargyl ethers is developed to provide the rapid construction of a fused polycyclic indenone-indole scaffold under mild conditions. The reaction proceeds via a highly ordered process involving Sonogashira coupling, propargyl-allenyl isomerization, allene-azide cycloaddition, denitrogenation, and diradical coupling. The proposed reaction mechanism is supported by experimental and computational studies.
View Article and Find Full Text PDFPoststroke Translocator Protein Expression Dynamics and Correlations to Chronic Infarction: A -CLINDE-SPECT Study.
J Neuroimaging
January 2025
Neurobiology Research Unit, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark.
Background And Purpose: This study aims to investigate the longitudinal changes in translocator protein (TSPO) following stroke in different brain regions and potential associations with chronic brain infarction.
Methods: Twelve patients underwent SPECT using the TSPO tracer 6-Chloro-2-(4'-123I-Iodophenyl)-3-(N,N-Diethyl)-Imidazo[1,2-a]Pyridine-3-Acetamide, as well as structural MRI, at 10, 41, and 128 days (median) after ischemic infarction in the middle cerebral artery. TSPO expression was measured in lesional (MRI lesion and SPECT lesion), connected (pons and ipsilesional thalamus), and nonconnected (ipsilesional cerebellum and contralesional occipital cortex) regions.
Longitudinal Serotonergic and Dopaminergic Binding: Impact on Parkinson's Disease Progression and Levodopa Dyskinesia.
J Neuroimaging
January 2025
Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seongnam-si, Republic of Korea.
Background And Purpose: We investigated the relationship between serotonergic and dopaminergic specific binding transporter ratios (SBRs) over 4 years in Parkinson's disease (PD) patients. We assessed serotonergic innervation's potential compensatory role for dopaminergic denervation, association with PD symptoms, and involvement in the development of levodopa-induced dyskinesia (LID).
Methods: SBRs of the midbrain and striatum were evaluated from [I-123] N-ω-fluoropropyl-2β-carbomethoxy-3β-(4-iodophenyl)nortropane SPECT images at baseline and after 4 years.
I-β-Methyl Iodophenyl Pentadecanoic Acid and Thallium Dual Myocardial Single-Photon Emission Computed Tomography (BMIPP/Tl SPECT) Detects Coronary Microvascular Dysfunction in a Patient With Antiphospholipid Syndrome Nephropathy.
Circ J
January 2025
Department of Radioisotope Medicine, Atomic Bomb Disease and Hibakusha Medicine Unit, Atomic Bomb Disease Institute, Nagasaki University.
A Water-Soluble Small Molecule Boron Carrier Targeting Biotin Receptors for Neutron Capture Therapy.
ACS Omega
December 2024
School of Life Science and Technology, Institute of Science Tokyo, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8501, Japan.
A critical challenge in boron neutron capture therapy (BNCT) is expanding its effectiveness through the development of novel boron agents with different mechanisms of action than the approved drug 4-borono-l-phenylalanine (BPA). In this study, we developed a small molecule boron carrier, biotinyl--dodecaborate conjugate with an iodophenyl moiety (BBC-IP), incorporating biotin as a ligand for biotin receptors overexpressed in various cancer cells, alongside an albumin ligand and boron source. BBC-IP exhibited high water solubility, minimal cytotoxicity, and superior cellular uptake compared to BPA in both human and mouse cancer cells.
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