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Updated: Aug 27, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Highly bioactive novel aryl-, benzyl-, and piperazine-selenoureas: synthesis, structural characterization and in
Ziad Moussa1, Ranem Kaddoura1, Haythem A Saadeh2
1Department of Chemistry, College of Science, United Arab Emirates University, P. O. Box 15551, Al Ain, United Arab Emirates.
Abstract:
Selenoureas are widespread as useful elements for constructing important species and biologically active molecules. Finding an efficient and straightforward method to prepare this motif and biologically screen derivatives thereof is crucial. Herein, we demonstrate the effectiveness of using ethanol as a solvent in the preparation of various substituted aryl-, benzyl-, and piperazine-selenoureas from isoselenocyanates and amines. The synthetic method includes mild reaction conditions, large substrate scope, and good isolated yields. Biological evaluation of the prepared products on MDA-MB-231 and MCF-7 cancer cell lines revealed several remarkably active compounds (IC50 < 10 μΜ) with the best one exhibiting IC50 values of 1.8 μΜ and 1.2 μΜ observed against the challenging former triple-negative breast cancer cell line and the latter one, respectively. The chemical structures of all new compounds were fully characterized by multinuclear nuclear magnetic resonance (NMR) spectroscopy and high accuracy mass measurements.
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