Topoisomerase II inhibitor 14 是一种有效的拓扑异构酶 II 抑制剂,具有抗癌活性和抗氧化活性。Topoisomerase II inhibitor 14 诱导细胞凋亡,并将细胞周期阻滞在 S 期。Topoisomerase II inhibitor 14 可降低 GSH、MDA 和 NO 的量。
Topoisomerase II inhibitor 4 (compound E17) 是一种拓扑异构酶 II (Topoisomerase II) 的有效抑制剂。Topoisomerase II inhibitor 4 具有抗肿瘤效果,能够将阻滞细胞周期于 G2 M 期,抑制癌细胞增殖并表现出细胞毒性。
Topoisomerase I II inhibitor 3 (化合物7) 是拓扑异构酶 I (Topo I)和 II (Topo II)的有效双抑制剂。 通过抑制 PI3K Akt mTOR 信号通路,Topoisomerase I II inhibitor 3抑制细胞增殖、侵袭和迁移,诱导细胞凋亡(apoptosis)。Topoisomerase I II inhibitor 3 在肝癌中具有研究价值。
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].
Topoisomerase I inhibitor 7 (Compound 8) 是有效的Topoisomerase I 抑制剂。Topoisomerase I inhibitor 7 显著抑制肿瘤生长(高达 79%)。在接受 P388 淋巴瘤移植的小鼠模型中,Topoisomerase I inhibitor 7延长了小鼠寿命(153%)。