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.

Topoisomerase inhibitor3 (compound 9) is an effective inhibitor of topoisomerase. This compound exhibits antiproliferative and antitumor activities.

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 14 (Compound 4h) acts as an inhibitor of topoisomerase I. It suppresses the proliferation of A549 and C6 cells, with IC50 values of 4.56 μM and 13.17 μM, respectively. The compound shows no significant toxicity towards healthy NIH3T3 cells (IC50 of 74.44 μM) and demonstrates anticancer activity.

TopoisomeraseI inhibitor 12 (compound 12) is a Camptothecin-derived compound and serves as a potent inhibitor of Topoisomerase I (TopoisomeraseI). This compound exhibits anticancer properties.

TopoisomeraseII inhibitor 17 (compound 4c) is a thiazolopyrimidine-based inhibitor of Topoisomerase II with an IC50 of 0.23 μM. This compound significantly disrupts the cell cycle and induces apoptosis.

TopoisomeraseI inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I, exhibiting anticancer properties. Its IC50 value against A549 cells is 7.34 μM.

Topoisomerase II inhibitor 19 (compound 5h) is a DNA intercalator and a topoisomerase II inhibitor with an IC50 of 0.34 μM. It induces damage in ctDNA.

Topoisomerase I inhibitor 21 (Compound 3e) inhibits Topoisomerase I by stabilizing the enzyme-DNA complex. It exhibits antiproliferative activity in 39 types of human cancer cells (JFCR39), with an average GI50 of 39 nM.

TopoisomeraseII inhibitor 20 (Compound 3e) is a potent inhibitor of Topoisomerase II, with an IC50 of 0.98 µM. It can induce apoptosis and possesses broad-spectrum anticancer activity.

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].