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ИСТИНА ЦЭМИ РАН |
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The invention relates to the field of organic and medicinal chemistry, as well as molecular biology, and concerns a new class of compounds for imaging PSMA expressing cells and tissues, such as prostate cancer cells. New diagnostic conjugates for the visualization of pathogenic cells or tissues expressing PSMA, including the PSMA ligand with a linker and a fluorescent dye, the method for its preparation and use are claimed. The technical result of the claimed group of inventions is the high affinity and selectivity of the action of the claimed conjugates in relation to PSMA expressing cells. These compounds allow you to expand the arsenal of diagnostic tools for imaging cells with high level of PSMA expression. The use of an azido derivative of aminopentanoic acid makes it possible to obtain a PSMA vector with a long hydrophobic linker and protected carboxy groups, which in turn facilitates its modification, increases the yield and reduces the amount of solvents used in the process due to a significant increase in the solubility of the starting compound (PSMA vector with a long hydrophobic linker and protected carboxy groups). The key feature of the claimed conjugate is the presence of a long hydrophobic linker in the structure, as well as additional aromatic fragments, the presence of which contributes to better binding of the claimed conjugate to the protein target, due to the involvement of additional interactions between the compound and the hydrophobic pockets in the structure of the hydrophobic tunnel of the protein target.