Abstract
A new series of 3,7-disubstituted coumarin derivatives were synthesized. Where treatment of 7-hydroxy-3-substituted coumarins (1a, b) with p-chlorophenacyl bromide afforded (E)-3-acetyl-7-(2-(4-chlorophenyl)-2-hydroxyvinyloxy)-2H-chromen-2-one (2) and ethyl 7-(2-(4-chlorophenyl)-2-oxoethoxy)-2-oxo-2H-chromene-3-carboxylate (3). The acetylation of compounds 2 and 3 with acetic anhydride in diverse conditions yielded acetyl derivatives (4 and 5). 7-hydroxy-2-oxo-N-p-tolyl-2H-chromene-3-carboxamide (6) and 7-(2-(4-chlorophenyl)-2-oxoethoxy)-2-oxo-N-p-tolyl-2H-chromene-3-carboxamide (7) was obtained via condensation of compound 1b or 3 with p-toluidine. Antitumor activities of the synthesized compounds were evaluated on human Hepatocellular cancer cell line (HePG2) and colon carcinoma (HCT-116) cell line. Among the synthesized compounds 2 and 4 have the highest activity against the tested cell lines.