M. J. Parulava, Yu. N. Kotovshchikov, G. V. Latyshev, D. V. Sokolova, I. P. Beletskaya, N. V. Lukashev, “Synthesis of novel cytotoxic 3-azolylsteroids via Cu-catalyzed C–N coupling”, Mendeleev Commun., 31:3 (2021), 359

Эта публикация цитируется в 2 статьях

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^a

^a 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

Аннотация: 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.

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

Язык публикации: английский

DOI: 10.1016/j.mencom.2021.04.025

	*Дополнительные материалы:*
		Supplementary_data_1.pdf	851.8 Kb