Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα/β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1].
TopoisomeraseI II inhibitor 6(compound 3i)作为topoisomerase I 和 II 的抑制剂显示出优异的效能,其IC50值分别为4.77 µM和 15 µM。此外,该化合物在人类黑色素瘤LOX IMVI癌细胞系中展示了显著的抗增殖效果,IC50值达到了26.7 µM和25.4 µM。
Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂,IC50值为 1.7 nM,并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性,IC50值为 0.98 μM。