Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor. Topo I-IN-1 exhibits antitumor activity and DNA intercalative capability. Topo I-IN-1 can induce cell apoptosis.

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 [1]. Topo I-IN-1 (0-4 μM, 48 h) shows a dose-dependent apoptotic effect, induces ROS generation, and inhibits cell migration [1]. Cell Cytotoxicity Assay [1] Cell Line: A549, HCT116, MCF7, SK-MEL-28, and NRK (normal rat kidney epithelial cells) Concentration: 0-50 μM Incubation Time: 48 h Result: Showed in vitro cytotoxicity with IC 50 values of 2.33 ± 1.52, 2.85 ± 0.83, 26.23 ± 2.48, 3.86 ± 0.33, and 29.99 ± 0.95 μM against A549, HCT116, MCF7, SK-MEL-28, and NRK cells, respectively. Apoptosis Analysis [1] Cell Line: A549 Concentration: 2, 2.33 and 4 μM Incubation Time: 48 h Result: Resulted in the morphological changes typical to apoptosis.