This article is cited in 3 papers

Communications

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

M. J. Parulava^a, Yu. N. Kotovshchikov^a, G. V. Latyshev^a, D. V. Sokolova^bc, I. P. Beletskaya^a, N. V. Lukashev<sup>a

a</sup> Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
^b N.N. Blokhin National Medical Research Center of Oncology, Moscow, Russian Federation
^c Peoples Friendship University of Russia (RUDN University), Moscow, Russian Federation

Abstract: 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 2.0–10.1μm.

Keywords: steroids, copper catalysis, nitrogen heterocycles, iodoalkenes, antiproliferative activity, MTT assay.

Language: English

DOI: 10.1016/j.mencom.2021.04.025

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