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Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.
Zyk, Nikolai Y; Ber, Anton P; Nimenko, Ekaterina A; Shafikov, Radik R; Evteev, Sergei A; Petrov, Stanislav A; Uspenskaya, Anastasia A; Dashkova, Natalia S; Ivanenkov, Yan A; Skvortsov, Dmitry A; Beloglazkina, Elena K; Majouga, Alexander G; Machulkin, Aleksei E.
Afiliación
  • Zyk NY; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation. Electronic address: Zyknikola@gmail.com.
  • Ber AP; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Nimenko EA; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Shafikov RR; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of Sciences, GSP-7, Ulitsa Miklukho-Maklaya, 16/10, Moscow 117997, Russian Federation.
  • Evteev SA; The Federal State Unitary Enterprise Dukhov Automatics Research Institute, Moscow, 127055, Russia.
  • Petrov SA; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Uspenskaya AA; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Dashkova NS; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Ivanenkov YA; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; The Federal State Unitary Enterprise Dukhov Automatics Research Institute, Moscow, 127055, Russia.
  • Skvortsov DA; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Beloglazkina EK; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Majouga AG; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; Dmitry Mendeleev University of Chemical Technology of Russia, Miusskaya Sq. 9, Moscow 125047, Russian Federation.
  • Machulkin AE; Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; RUDN University, Miklukho-Maklaya Str. 6, Moscow 117198, Russian Federation.
Bioorg Med Chem Lett ; 71: 128840, 2022 09 01.
Article en En | MEDLINE | ID: mdl-35661685
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 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Neoplasias de la Próstata / Lisina Límite: Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Neoplasias de la Próstata / Lisina Límite: Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article Pais de publicación: Reino Unido