Bioorganic and Medicinal Chemistry Letters, volume 71, pages 128840

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

Zyk Nikolai Y. 1
Ber Anton P 1
Nimenko Ekaterina A. 1
Shafikov Radik R 1, 2
Dashkova Natalia S 1
Ivanenkov Yan 1, 3
Publication typeJournal Article
Publication date2022-09-01
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor2.7
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
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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Zyk N. Y. et al. Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom // Bioorganic and Medicinal Chemistry Letters. 2022. Vol. 71. p. 128840.
GOST all authors (up to 50) Copy
Zyk N. Y., Ber A. P., Nimenko E. A., Shafikov R. R., Evteev S. A., Petrov S. B., Uspenskaya A. A., Dashkova N. S., Ivanenkov Y., Skvortsov D., Beloglazkina E. K., Majouga A. G., Machulkin A. E. Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom // Bioorganic and Medicinal Chemistry Letters. 2022. Vol. 71. p. 128840.
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TY - JOUR
DO - 10.1016/j.bmcl.2022.128840
UR - https://doi.org/10.1016%2Fj.bmcl.2022.128840
TI - Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Zyk, Nikolai Y.
AU - Ber, Anton P
AU - Nimenko, Ekaterina A.
AU - Shafikov, Radik R
AU - Evteev, Sergei A
AU - Petrov, Stanislav B.
AU - Uspenskaya, Anastasia A.
AU - Dashkova, Natalia S
AU - Ivanenkov, Yan
AU - Skvortsov, Dmitry
AU - Beloglazkina, Elena K.
AU - Majouga, Alexander G.
AU - Machulkin, Aleksei E.
PY - 2022
DA - 2022/09/01 00:00:00
PB - Elsevier
SP - 128840
VL - 71
SN - 0960-894X
SN - 1464-3405
ER -
BibTex
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BibTex Copy
@article{2022_Zyk
author = {Nikolai Y. Zyk and Anton P Ber and Ekaterina A. Nimenko and Radik R Shafikov and Sergei A Evteev and Stanislav B. Petrov and Anastasia A. Uspenskaya and Natalia S Dashkova and Yan Ivanenkov and Dmitry Skvortsov and Elena K. Beloglazkina and Alexander G. Majouga and Aleksei E. Machulkin},
title = {Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2022},
volume = {71},
publisher = {Elsevier},
month = {sep},
url = {https://doi.org/10.1016%2Fj.bmcl.2022.128840},
pages = {128840},
doi = {10.1016/j.bmcl.2022.128840}
}
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