Summary: | Scientists have been interested in hybrid coumarin derivatives due to their wide clinical anticancer use. Herein, ethyl 8-methoxycoumarin-3-carboxylate (Compound <b>1</b>) served as the starting material for the synthesis of a series of novel hybrid coumarin derivatives (Compounds <b>3</b>–<b>6</b>). Their structure was determined using <sup>13</sup>C NMR, <sup>1</sup>H NMR, elemental analysis, and mass spectrometry. The in vitro cytotoxic activities of coumarin derivatives (Compounds <b>3</b>, <b>5</b>, and <b>6</b>) and brominated coumarin derivatives (Compounds <b>4</b>, <b>8</b>, and <b>9</b>) against MCF-7 and MDA-MB-231 were evaluated. Several substances have been identified as promising candidates for future study, especially Compound <b>6</b> due to its potent activity against β-tubulin (TUB) polymerization, sulfatase, and aromatase enzymes. It also has a role in inducing cell-cycle arrest at the S phase in the MCF-7 cell line, as well as apoptosis.
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