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

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. © 2022 Elsevier Ltd

Authors
Zyk N.Y.1 , Ber A.P.1 , Nimenko E.A.1 , Shafikov R.R.1, 2 , Evteev S.A.3 , Petrov S.A.1 , Uspenskaya A.A.1 , Dashkova N.S.1 , Ivanenkov Y.A.1, 3 , Skvortsov D.A.1 , Beloglazkina E.K.1 , Majouga A.G.1, 4 , Machulkin A.E. 1, 5
Journal
Bioorganic and Medicinal Chemistry Letters
Publisher
Elsevier Ltd
Language
English
Status
Published
Link
External link
DOI
10.1016/j.bmcl.2022.128840
Number
128840
Volume
71
Year
2022
Organizations
  • 1 Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow, 119991, Russian Federation
  • 2 Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of Sciences, GSP-7, Ulitsa Miklukho-Maklaya, 16/10, Moscow, 117997, Russian Federation
  • 3 The Federal State Unitary Enterprise Dukhov Automatics Research Institute, Moscow, 127055, Russian Federation
  • 4 Dmitry Mendeleev University of Chemical Technology of Russia, Miusskaya Sq. 9, Moscow, 125047, Russian Federation
  • 5 RUDN University, Miklukho-Maklaya Str. 6, Moscow, 117198, Russian Federation
Keywords
Drug delivery; Ligands; Prostate cancer; Prostate-specific membrane antigen; Sulfo-Cy5
Date of creation
06.07.2022
Date of change
06.07.2022
Short link
https://repository.rudn.ru/en/records/article/record/83524/
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