1. Influence of the dipeptide linker configuration on the activity of PSMA ligands
- Author
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Dmitry A. Skvortsov, Alexey E. Machulkin, Elena K. Beloglazkina, Stanislav A. Petrov, Alexander G. Majouga, Anastasiya A. Uspenskaya, Radik R. Shafikov, and Ekaterina A. Nimenko
- Subjects
In vitro test ,Dipeptide ,010405 organic chemistry ,Stereochemistry ,Phenylalanine ,General Chemistry ,010402 general chemistry ,Cleavage (embryo) ,01 natural sciences ,0104 chemical sciences ,chemistry.chemical_compound ,chemistry ,Glutamate carboxypeptidase II ,Urea ,Tyrosine ,Linker - Abstract
Selective ligands of an urea-based prostate specific membrane antigen with a phenylalanine/tyrosine-based dipeptide linker and with a mingled chiral centers configuration and/or substituted aromatic fragments were prepared in seven steps by liquid- and in six steps by solid-phase synthesis. In vitro test for inhibiting the cleavage of N-acetylaspartylglutamate revealed the optimum linker containing l -phenylalanine in the structure on the N-terminus of a dipeptide chain.
- Published
- 2020
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