Discovery and cytotoxic activity of N-CF3-containing pyrroloindolines

Pyrroloindoline scaffolds are widely found in numerous biologically active and medicinally significant natural products. Meanwhile, the potential applications of N -CF ₃ compounds in medicinal chemistry have garnered increasing attention due to their unique properties. However, the pharmacological activities and therapeutic potential of N -CF ₃ -containing pyrroloindolines remain underexplored. Building on our previously developed method for constructing N -CF ₃ -containing pyrroloindoline scaffolds, this study systematically evaluated the antitumor activities of a diverse series of N -CF₃-containing pyrroloindoline derivatives. Cell-based assays demonstrated that these derivatives exhibited significant antiproliferative activities against human cancer cell lines, including 786-O, A498, and HepG2. Further investigations revealed that N -CF ₃ -containing pyrroloindolines not only induce apoptosis in cancer cells but also inhibit colony formation. Moreover, they showed potential to suppress cancer cell metastasis and proliferation, primarily by inducing apoptosis and cell cycle arrest. These findings suggest that N -CF ₃ -containing pyrroloindolines hold great promise as potential anticancer agents and merit further development.