Double-Armed 18- and 21-Membered Macrocycles as Potential Chelators for Lead and Bismuth Radiopharmaceuticals.

With increasing clinical applications and interest in targeted alpha therapy, there is growing interest in developing alternative chelating agents for [Pb]Pb and [Bi]Bi that exhibit rapid radiolabeling kinetics and kinetic inertness. Herein we report the synthesis and detailed investigation of diacetate and dipicolinate 18- and 21-membered macrocyclic chelators BADA-18, BADA-21, BADPA-18, and BADPA-21 for the complexation of Pb and Bi ions with potential use in the preparation of radiopharmaceuticals. The formation of mononuclear complexes was established by using ESI-mass spectrometry, and their stability constants were determined by potentiometric titration.

Synthesis of new acyclic chelators H4aPyta and H6aPyha and their complexes with Cu, Ga, Y, and Bi.

In this article, we present the synthesis and characterization of new acyclic pyridine-containing polyaminocarboxylate ligands H4aPyta and H6aPyha, which differ in structural rigidity and the number of chelating groups. Their abilities to form complexes with Cu, Ga, Y, and Bi cations, as well as the stability of the complexes, were evaluated by potentiometric titration method, radiolabeling with the corresponding radionuclides, studies, mass spectrometry, and HPLC. The structures of the resulting complexes were determined using NMR spectroscopy and DFT calculations.

Insights into Actinium Complexes with Tetraacetates─AcBATA versus AcDOTA: Thermodynamic, Structural, and Labeling Properties.

In the current research, we conducted a comparative study of the Ac complex with HDOTA and HBATA. The stability constants of the [AcBATA] and [AcDOTA] complexes were studied directly by extraction methods. We discovered that the thermodynamic properties of the [AcBATA] complex are superior to those of [AcDOTA].

DTPA(DOTA)-Nimotuzumab Radiolabeling with Generator-produced Thorium for Radioimmunotherapy of EGFR-overexpressing Carcinomas.

Introduction: The feasibility of preparing the "in-house" generators and the Th- DTPA(DOTA)-Nimotuzumab radioimmunoconjugate was evaluated. Th is perspective for TAT, however, due to short half-life it is preferable to apply this radionuclide for readily available epithelial malignancies. Nimotuzumab being specific for EGFR expressing cells as a targeting moiety is considered to be suitable for thorium delivery.

Plier Ligands for Trapping Neurotransmitters into Complexes for Sensitive Analysis by SERS Spectroscopy.

Catecholamines-dopamine, noradrenaline and adrenaline are important biomarkers of neurotransmitter metabolism, indicating neuroendocrine tumors and neurodegenerative diseases. Surface-enhanced Raman spectroscopy (SERS) is a promising analytical technique with unprecedented multiplexing capabilities. However, not all important analytes exhibit strong SERS signals on stable and robust nanostructured substrates.

Novel Hybrid Benzoazacrown Ligand as a Chelator for Copper and Lead Cations: What Difference Does Pyridine Make.

A synthetic procedure for the synthesis of azacrown ethers with a combination of pendant arms has been developed and the synthesized ligand, characterized by various techniques, was studied. The prepared benzoazacrown ether with hybrid pendant arms and its complexes with copper and lead cations were studied in terms of biomedical applications. Similarly to a fully acetate analog, the new one binds both cations with close stability constants, despite the decrease in both constants.

Pb: Production Approaches and Targeted Therapy Applications.

Over the last decade, targeted alpha therapy has demonstrated its high effectiveness in treating various oncological diseases. Lead-212, with a convenient half-life of 10.64 h, and daughter alpha-emitter short-lived Bi ( = 1 h), provides the possibility for the synthesis and purification of complex radiopharmaceuticals with minimum loss of radioactivity during preparation.

Labeling and receptor affinity of an ultra-short somatostatin analogue Thz-Phe-D-Trp-Lys-Thr-DOTA.

Somatostatin analogues play an important role in the therapy of neuroendocrine tumors by binding to somatostatin receptors on the surface of cancer cells. In this work, we analyze the receptor-binding affinity and in vitro stability of a novel ultra-short somatostatin analogue Thz-Phe-D-Trp-Lys-Thr-DOTA (DOTA-P4). This conjugate is successfully radiolabeled with Sc, Y, Eu, and Bi, characterized and validated by thin layer and high-performance liquid chromatography.

Zinc and copper complexes with azacrown ethers and their comparative stability in vitro and in vivo.

Copper-based radiopharmaceuticals are of high interest these days owing to the decay properties of copper radioisotopes. In contrast, labeled zinc compounds have been less studied for applications in nuclear medicine. In this study, the stability of labeled zinc and copper complexes with two azacrown ether ligands was investigated and compared.

Benzoazacrown compound: a highly effective chelator for therapeutic bismuth radioisotopes.

A new benzoazacrown ligand HBATA was synthesized and its complexation ability towards bismuth cations was evaluated. Binding of cation occurs at room temperature in a few minutes and formed complex exhibits the same level of inertness as highly stable complex with the well-known in biologically relevant and challenging media under conditions.

From octreotide to shorter analogues: Synthesis, radiolabeling, stability.

This study aims at analyzing complexation properties of two new short somatostatin analogues, their synthesis, radiolabeling with Sc, Bi, and Eu and stability in vitro. Short tetrapeptide Phe-d-Trp-Lys-Thr and pentapeptide Thz-Phe-d-Trp-Lys-Thr were first conjugated with the DOTA macrocyclic chelator. These conjugates were radiolabeled with Sc, Bi, and Eu and characterized by thin-layer chromatography (TLC) and HPLC.

Copper-Bispidine Complexes: Synthesis and Complex Stability Study.

A new series of dicarboxylic derivatives of bispidines have been synthesized to develop novel copper(II) complexes suitable as imaging agents for positron emission tomography. For characterization purposes, copper complexes of bispidines were synthesized in the pure form and in quantitative yields by neutralization of ligands with malachite. The formation of complexes and their stoichiometries were studied by potentiometric titration, cyclic voltammetry, and spectroscopic methods.