The present invention discloses a PSMA-targeted radiometal complex containing a nitroaromatic heterocyclic group and its preparation, which belongs to the technical fields of radiopharmaceuticals and
medical imaging. The general formula of the PSMA-targeted radiometal complex containing a nitroaromatic heterocyclic group of the present invention is shown in Formula I and Formula II. The present invention is the first to link both a nitroaromatic group and a PSMA-targeting group to a
metal chelator (such as HBED-CC,
DOTA,
DOTA(GA)2, NOTA, AAZTA, etc.) and to target a radiometal
nuclide, e.g. 68 Ga, 18 F-AlF, 177 Lu, 90 Y, 44 Sc, 225 Ac, 212 Pb, 213 The radioactive
metal marker is labeled with Bi, etc. The synergistic effect of the nitroaromatic heterocyclic group
in vivo is expected to increase the uptake of the radioactive
metal marker by
prostate cancer, promoting
metabolism in non-target organs and improving the therapeutic
efficacy of radiopharmaceuticals against tumors.
JPEG2026508753000106.jpg2835
JPEG2026508753000107.jpg2145 (wherein the R1 and R2 groups are nitroaromatic heterocyclic groups; L2 is a linking group between the R1 group and L1, where L1 is a linking group between the chelator and the structure PSMA targeting structure; L4 is a linking group between the R2 group and L3, where L3 is a linking group between the chelator and the structure PSMA targeting structure; and ChelatoR1 and ChelatoR2 are chelators or chelating structures.)