Moussa Ziad, Kaddoura Ranem, Saadeh Haythem A, Abutaha Nael, Ahmed Saleh A
Department of Chemistry, College of Science, United Arab Emirates University, P. O. Box 15551, Al Ain, United Arab Emirates.
Department of Chemistry, School of Science, The University of Jordan, Amman 11942, Jordan.
Heliyon. 2022 Sep 21;8(9):e10709. doi: 10.1016/j.heliyon.2022.e10709. eCollection 2022 Sep.
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 (IC < 10 μΜ) with the best one exhibiting IC 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.
硒脲作为构建重要物种和生物活性分子的有用元素广泛存在。找到一种高效且直接的方法来制备该结构单元并对其衍生物进行生物筛选至关重要。在此，我们证明了在由异硒氰酸酯和胺制备各种取代的芳基、苄基和哌嗪基硒脲时使用乙醇作为溶剂的有效性。该合成方法包括温和的反应条件、广泛的底物范围和良好的分离产率。对制备的产物在MDA-MB-231和MCF-7癌细胞系上进行的生物学评价显示了几种具有显著活性的化合物（IC<10μM），其中最佳的化合物对具有挑战性的前者三阴性乳腺癌细胞系和后者分别表现出1.8μM和1.2μM的IC值。所有新化合物的化学结构均通过多核核磁共振（NMR）光谱和高精度质量测量进行了全面表征。
