Synthesis of novel cytotoxic 3-azolylsteroids via Cu-catalyzed C–N coupling

A series of novel 3-azolylandrosta-3,5-dienes was prepared via Cu-catalyzed Ullmann C–N coupling between a readily available steroidal vinyliodide and a variety of NH-heterocycles. The cytotoxic activity of the target compounds was evaluated against selected cancer cell lines (MCF-7, SKOV-3, DU-145, PC-3). Compound bearing gramine fragment showed the highest antiproliferative effect with IC50 values in the range of 2.0–10.1 μm. © 2021

Authors
Parulava M.J.1 , Kotovshchikov Y.N.1 , Latyshev G.V.1 , Sokolova D.V. 2, 3 , Beletskaya I.P.1 , Lukashev N.V.1
Journal
Mendeleev Communications
Publisher
Royal Society of Chemistry
Number of issue
3
Language
English
Pages
359-361
Status
Published
Link
External link
DOI
10.1016/j.mencom.2021.04.025
Volume
31
Year
2021
Organizations
  • 1 Department of Chemistry, M. V. Lomonosov Moscow State University, Moscow, 119991, Russian Federation
  • 2 Peoples Friendship University of Russia (RUDN University), Moscow, 117198, Russian Federation
  • 3 N. N. Blokhin National Medical Research Center of Oncology, Moscow, 115478, Russian Federation
Keywords
antiproliferative activity; copper catalysis; iodoalkenes; MTT assay; nitrogen heterocycles; steroids
Date of creation
20.07.2021
Date of change
20.07.2021
Short link
https://repository.rudn.ru/en/records/article/record/74303/
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