Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.
Bioorg Med Chem Lett
; 71: 128840, 2022 09 01.
Article
em En
| MEDLINE
| ID: mdl-35661685
ABSTRACT
We report an improved series of ligands targeting prostate specific membrane antigen (PSMA). The new compounds were designed by the introduction of changes in the structure of the aromatic fragment at ε-nitrogen atom of lysine that resulted in improved biological parameters. Some of them demonstrated high selectivity and nanomolar IC50 values. We synthesized and tested two conjugates with a fluorescent label Sulfo-Cy5 as an example of the use of the obtained PSMA inhibitors as a basis for the creation of diagnostic preparations.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Próstata
/
Lisina
Limite:
Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2022
Tipo de documento:
Article