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Phuong, Tran Hoang
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article
Synthesis, structure and <i>in vitro</i> cytotoxicity testing of some 2-aroylbenzofuran-3-ols
Abstract
<jats:p>Five 2-aroyl-5-bromobenzo[<jats:italic>b</jats:italic>]furan-3-ol compounds (two of which are new) and four new 2-aroyl-5-iodobenzo[<jats:italic>b</jats:italic>]furan-3-ol compounds were synthesized starting from salicylic acid. The compounds were characterized by mass spectrometry and <jats:sup>1</jats:sup>H NMR and <jats:sup>13</jats:sup>C NMR spectroscopy. Single-crystal X-ray diffraction studies of four compounds, namely, (5-bromo-3-hydroxybenzofuran-2-yl)(4-fluorophenyl)methanone, C<jats:sub>15</jats:sub>H<jats:sub>8</jats:sub>BrFO<jats:sub>3</jats:sub>, (5-bromo-3-hydroxybenzofuran-2-yl)(4-chlorophenyl)methanone, C<jats:sub>15</jats:sub>H<jats:sub>8</jats:sub>BrClO<jats:sub>3</jats:sub>, (5-bromo-3-hydroxybenzofuran-2-yl)(4-bromophenyl)methanone, C<jats:sub>15</jats:sub>H<jats:sub>8</jats:sub>Br<jats:sub>2</jats:sub>O<jats:sub>3</jats:sub>, and (4-bromophenyl)(3-hydroxy-5-iodobenzofuran-2-yl)methanone, C<jats:sub>15</jats:sub>H<jats:sub>8</jats:sub>BrIO<jats:sub>3</jats:sub>, were also carried out. The compounds were tested for their <jats:italic>in vitro</jats:italic> cytotoxicity on the four human cancer cell lines KB, Hep-G2, Lu-1 and MCF7. Six compounds show good inhibiting abilities on Hep-G2 cells, with IC<jats:sub>50</jats:sub> values of 1.39–8.03 µ<jats:italic>M</jats:italic>.</jats:p>