DNA topoisomerase II inhibitor 1

DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

DNA topoisomerase II inhibitor 1 (compound 8ed) (0-10 µM; 48 h) shows cytotoxic activity with IC50s of 10.10, >10, 0.59, 4.20, >10, >10, 8.41 µM for HT-29, MDA-MB-231, MG-63, U87MG, PC3, HeLa, Vero cells, respectively[1]. DNA topoisomerase II inhibitor 1 (0.5, 2 µM; 24 h) induces apoptosis and cell cycle arrest at sub G1 phase[1]. DNA topoisomerase II inhibitor 1 (0.5, 2 µM) increases the generation of reactive oxygen species (ROS)[1].

[1]. Lakshmi Manasa K, et al. Design and synthesis of β-carboline linked aryl sulfonyl piperazine derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability. Bioorg Chem. 2020 Aug;101:103983.