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[Tc]Technetium and Rhenium Dithiocarbazate Complexes: Chemical Synthesis and Biological Assessment.
Pharmaceutics
January 2025
Laboratory of Nuclear Medicine (LIM-43), Hospital das Clinicas HCFMUSP, Faculdade de Medicina, Universidade de Sao Paulo, Sao Paulo 05403-911, SP, Brazil.
Background/objectives: Dithiocarbazates (DTCs) and their metal complexes have been studied regarding their property as anticancer activities. In this work, using S-benzyl-5-hydroxy-3-methyl-5-phenyl-4,5-dihydro-1H-pirazol-1-carbodithionate (Hbdtc), we prepared [ReO(bdtc)(Hbdtc)] and [[Tc]TcO(bdtc)(Hbdtc)] complexes for tumor uptake and animal biodistribution studies.
Methods: Re complex was prepared by a reaction of H2bdtc and (NBu)[ReOCl], the final product was characterized by IR, H NMR, CHN, and MS-ESI.
Novel technetium-99m-labelled ribociclib isocyanide derivatives for imaging cyclin-dependent kinase 4/6 (CDK4/6) expression in cancer.
Eur J Med Chem
January 2025
Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing, 100875, China. Electronic address:
Cyclin-dependent kinase 4/6 (CDK4/6) plays a crucial role in cell cycle regulation, is overexpressed in various cancers and is an important target in the development of radiotracers for tumour imaging. Despite the increasing recognition of CDK4/6 inhibitors in cancer therapy, their application is limited by the lack of suitable biomarkers. Herein, we developed a series of technetium-99m-labelled CDK4/6 radiotracers and utilized a linker optimization strategy to reduce their abdominal uptake and enhance their imaging properties.
View Article and Find Full Text PDFSentinel lymph nodes biopsy for malignant tumors using Technefit radioactive colloid Technetium Tc.
Folia Med (Plovdiv)
December 2024
Botkin Hospital, Moscow, Russia.
Technetium-99m (99mTc) is a short-lived nanocolloid nuclide widely used by oncologists to diagnose and identify cancer dissemination.
View Article and Find Full Text PDFOdd-Numbered Ring Cluster Tc(μ-O)Cl(OOCCCl): Synthesis, Crystal Structure, and Optical and Thermal Properties.
Inorg Chem
December 2024
Frumkin Institute of Physical Chemistry and Electrochemistry, Russian Academy of Sciences, Leninsky prosp. 31-4, 119071 Moscow, Russia.
Herein, we report a method for the preparation of the first odd homometallic and heterovalent nine-centered Tc wheel, [Tc(μ-O)Cl(OOCCl)]. The synthesized compound represents the pioneering instance of such clusters among d elements and is the fourth instance observed across all metals. The ring was synthesized by a solvothermal method in a solution of technetium acid in trichloroacetic anhydride.
View Article and Find Full Text PDFSynthesis and Evaluation of Tc-Labeled l-Aspartic Acid as a EuK Polymer Linker for Targeting PSMA to a Novel SPECT Tumor Tracer.
J Med Chem
December 2024
Key Laboratory of Radiopharmaceuticals of the Ministry of Education, College of Chemistry, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), Beijing Normal University, Beijing 100875, P. R. China.
The development of novel tracers targeting prostate-specific membrane antigen (PSMA) has great potential for improving the diagnosis and treatment of prostate cancer (PCa). This study aimed to improve the absolute tumor uptake and tumor-to-background ratios (TBRs) of this novel PSMA tracer by increasing the number of pharmacophores, Glu-urea-Lys (EuK), that specifically bind to PSMA. We successfully synthesized four radioligands and prepared a total of 12 stable radiotracers by coordinating Tc with various coligands.
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