topoisomerase inhibitor

Topoisomerase inhibitor4 (compound 45) acts as an effective inhibitor of Topoisomerase1 2, arresting the cell cycle at the G2 M phase and inducing Apoptosis. This compound exhibits potent antitumor activity.

Topoisomerase inhibitor 5 (compound 158) is an inhibitor of bacterial topoisomerase, with a minimum inhibitory concentration of 0.125 μg mL, and exhibits anti-tuberculosis activity.

Type II topoisomerase inhibitor 1 is a potent and selective inhibitor of E. coli DNA gyrase with an IC50 value of 1.7 nM and forms hydrogen bonds with the Asp73 residue. It inhibits topoisomerase IV activity with an IC50 value of 0.98 μM and is applicable in the antibacterial area [1] [2].

Topoisomerase Inhibitor 2 (18C) is a broad-spectrum bacterial topoisomerase inhibitor effective against multidrug-resistant Gram-negative bacteria [1].

Topoisomerase II inhibitor 13 inhibits topoisomerase II (Topo II) that shows strong anti-proliferation activity against HL-60 MX2 cancer cells derived from HL-60 against Topo II toxicity.

TopoisomeraseI II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.

TopoisomeraseII Inhibitor 20 TFA is a potent inhibitor of topoisomerase II with an IC50 of 0.98 µM. It can induce cell apoptosis and exhibits broad-spectrum anticancer activity.

Compound 5h (Topoisomerase I II inhibitor 7) is a Topoisomerase I II inhibitor.

Topoisomerase I inhibitor 2 (ZML-8) is a highly selective DNA topoisomerase I (Top1) inhibitor that impedes Top1 activity, causing DNA damage. It arrests the cell cycle at the G2 M phase and induces apoptosis, exhibiting anti-tumor effects [1].

Topoisomerase I (Compound ZML-14) inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2 M phase. Topoisomerase I inhibitor 3 is an inhibitor of topoisomerase I that interact with topoisomerase I-DNA complex [1].

Topoisomerase II inhibitor 8 (compound 22) is a potent inhibitor of topoisomerase II (IC50 = 0.52 μM) [1] and exhibits strong anti-proliferative activities, arresting the cell cycle at the G2 M phase.

Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective topoisomerase II inhibitor that blocks the CCRF-CEM cell cycle in the G2 phase and induces DNA double-strand breaks (DSB). It exhibits antiproliferative activity on various tumor cell lines and has potential for cancer research [1].

Topoisomerase I II inhibitor 2 (compound 1a) is a DNA topoisomerase I II dual inhibitor that significantly reduces xenograft tumor growth in a mouse model, indicating its potential use in treating liver cancer. It is a potent topoisomerase inhibitor with IC50 values of 6.83 μM and 9.82 μM for LM9 cells and Huh7 cells [1].

Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative acting as a Type II DNA topoisomerase (topo II) inhibitor. It specifically targets topo IIα β subtypes, with IC50 values of 0.17 μM for topo IIα and 0.23 μM for topo IIβ, causing significant DNA damage and inducing apoptosis by triggering the loss of mitochondrial membrane potential [1].

Topoisomerase I inhibitor 5 is an efficient topoisomerase I inhibitor with an IC50 value, effectively disrupting DNA and inhibiting topoisomerase I activity. It induces apoptosis in MCF-7 cells and arrests the cell cycle at the G1 phase, displaying potency in reversing P-gp-mediated resistance to Adriamycin [1].

Topoisomerase I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity, effectively inhibiting the proliferation of various cancer cell lines, including HepG2, A549, MCF-7, and HeLa, with IC50 values of 1.20 μM, 2.09 μM, 1.56 μM, and 1.92 μM, respectively. Thus, Topoisomerase I inhibitor 4 holds promise for cancer research applications [1].

Topoisomerase I II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) that inhibits the PI3K Akt mTOR signaling pathway, subsequently inhibiting cell proliferation, invasion, and migration, and inducing apoptosis. This compound has research value in liver cancer.

Topoisomerase I inhibitor 7 (Compound 8) is a potent Topoisomerase I inhibitor that significantly reduces tumor growth by up to 79% and extends the lifespan of mice bearing P388 lymphoma transplants by 153%.

Topoisomerase I inhibitor 6 (Compound 3) is a potent Topoisomerase I inhibitor that traps the DNA-Top1 cleavage complex and exhibits low cytotoxicity in non-cancerous cell lines, making it valuable for research.

Topoisomerase I inhibitor 8, a hexacyclic analogue of camptothecin, is also a potent inhibitor of topoisomerase I and is toxic to tumour cells.

Topoisomerase II inhibitor 4 (compound E17) is a potent topoisomerase II inhibitor with antitumor effects, blocking the cell cycle in the G2 M phase, inhibiting cancer cell proliferation, and exhibiting cytotoxicity.

Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer properties.

Topoisomerase II inhibitor 9 is a Topo II inhibitor (IC50: 0.97 μM) and DNA embedding agent (IC50: 43.51 μM) that blocks the Hep G-2 cell cycle in the G2 M phase and induces apoptosis.

DNA topoisomerase II inhibitor 1 is a potent inhibitor of DNA topoisomerase II that arrests the cell cycle in sub-G1 phase and induces apoptosis with anti-value-added effects.