Anticancer Potential of 1 <i>H</i> ‐Indol‐3‐yl‐N‐Phenylacetamide Derivatives: Synthesis, Cytotoxic Evaluation, Apoptosis, and Molecular Docking Studies

Abstract A series of 1 H ‐indol‐3‐yl‐ N ‐phenylacetamide derivatives ( F1‐14 ) were synthesized through a one‐pot, multi‐component Ugi reaction. The compounds were evaluated as anticancer agents against human breast MCF‐7, human lung A549, and human ovarian SKOV3 cancer cell lines. promising results were obtained by C‐4 chloro and C‐4 bromo‐containing derivatives ( F4 and F5 ) against all tested cell lines with good results against MCF‐7 cancer cells (IC 50 = 12.97 and 10.62 µM, respectively). All compounds exhibited a higher selectivity index (SI) than doxorubicin. Further assessment by flow cytometry analysis showed strong apoptotic cell death induced by the most potent compound F5 in MCF‐7 cancer cells. Molecular docking studies strongly confirmed the experimental findings and revealed possible binding modes of these derivatives in the active site of antiapoptotic protein, Bcl‐xL (Figure ).