In Vitro: Topo I-IN-1 (Compound 14d) (0-50 µM, 48 h) shows antiproliferative activity against human cancer cells and has low toxicity toward normal rat kidney epithelial cells. Topo I-IN-1 (0-4 µM, 48 h) shows a dose-dependent apoptotic effect, induces ROS generation, and inhibits cell migration.