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Design, synthesis and anticancer activity of new benzofuran-chalcone hybrids and their water soluble sodium salts
(Wiley-v C H Verlag Gmbh, 2023-03-06) Coskun, Demet; Coşkun, Mehmet Fatih; Çınar-Asa, Sibel; Akgün, Oğuzhan; Akgün, Halime; Arı, Ferda; ARI, FERDA; Bursa Uludağ Üniversitesi/Fen Edebiyat Fakültesi/Biyoloji Bölümü.; 0000-0002-8410-1786; 0000-0002-2048-3252; 0000-0002-6729-7908; A-5608-2019; ADX-9980-2022; AAG-7012-2021
In this study, firstly, 1-(7-ethoxy-1-benzofuran-2-yl) ethanone and 1,1'-(7-ethoxy-1-benzofuran-2,4-diyl)diethanone were synthesized for the starting reagent purposes. The synthesized benzofuran-chalcone salts were soluble in water at room temperature. Structural analysis of the synthesized compounds was characterized by elemental analysis, FT-IR and NMR spectroscopy techniques. The anticancer activities of the compounds were determined by SRB viability assay in human lung cancer (A549, H1299) and breast cancer (MCF-7, MDA-MB-231) cell lines. Findings for apoptosis were determined by flow cytometry analysis and the PARP-ELISA method. The results of the in vitro SRB analysis of the compounds showed that some of the chalcone hybrids were very effective on both types of cancer in a dose and time-dependent manner. Treatment of all cancer cell types with these hybrids resulted in a significant increase in the percentage of early and mainly late apoptotic cells, demonstrating their apoptosis-inducing effects via the Caspase 3/7 Activity.