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. 2022 Sep 1:71:128840.
doi: 10.1016/j.bmcl.2022.128840. Epub 2022 May 31.

Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom

Nikolai Y Zyk  1 , Anton P Ber  2 , Ekaterina A Nimenko  2 , Radik R Shafikov  3 , Sergei A Evteev  4 , Stanislav A Petrov  2 , Anastasia A Uspenskaya  2 , Natalia S Dashkova  2 , Yan A Ivanenkov  5 , Dmitry A Skvortsov  2 , Elena K Beloglazkina  2 , Alexander G Majouga  6 , Aleksei E Machulkin  7
Affiliations

Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom

Nikolai Y Zyk et al. Bioorg Med Chem Lett. .

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.

Keywords: Drug delivery; Ligands; Prostate cancer; Prostate-specific membrane antigen; Sulfo-Cy5.

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