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 mu M.

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
DOI
10.1016/J.MENCOM.2021.05.025
Volume
31
Year
2021
Organizations
  • 1 Moscow MV Lomonosov State Univ, Dept Chem, Moscow 119991, Russia
  • 2 Peoples Friendship Univ Russia, RUDN Univ, Moscow 117198, Russia
  • 3 NN Blokhin Natl Med Res Ctr Oncol, Moscow 115478, Russia
Keywords
steroids; copper catalysis; nitrogen heterocycles; iodoalkenes; antiproliferative activity; MTT assay
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