Laboratory for the development of chelators and their conjugates with vector molecules for the production of radiopharmaceuticals

The synthesis and investigation of the properties of new complexons capable of effectively binding metal cations is an extremely urgent task of both fundamental and practical importance. Complexons are widely used in many fields of science and technology, ranging from analytical chemistry to medicines. For example, complexes with lanthanides are used as contrast agents for magnetic resonance imaging and fluorescent probes; complexes with radionuclides are used for the diagnosis and therapy of cancer; zinc, copper and lanthanide complexes mimic hydrolytic and antioxidant enzymes; free ligands are used as agents for chelation therapy in heavy metal poisoning; ligands containing chromophores fragments act as chemosensors for various cations and anions. Therefore, an important task in this field is to obtain complexons that demonstrate high selectivity of complexation, rapid metal cation binding, mild conditions for obtaining complexes, high stability constants, and kinetic inertia of complexes, especially in a biological environment. Our laboratory is developing new macrocyclic and acyclic complexes for heavy metal cations and radionuclides. The idea of our work is to obtain such chelators, in the structure of which a rigid and flexible fragment are combined, which makes it possible to combine their advantages in one molecule, namely, rapid complexation and stability of the formed complex. The structure of chelators varies between rigid aromatic fragments of benzene and pyridine, the number and nature of nitrogen and oxygen heteroatoms, the size of the macrocyclic cavity, the length of the polyamine chain, the number and type of chelating groups. In the course of comprehensive research, we identify the advantages and disadvantages of new ligands and identify patterns that affect the ability to bind a particular metal cation.