Topoisomerase II inhibitor 14 is a potent topoisomerase II inhibitor with anticancer and antioxidant activities.Topoisomerase II inhibitor 14 induces apoptosis and blocks the cell cycle in S phase.Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO. Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO.

Topoisomerase I Inhibitor 9 (compound 3d), a specific inhibitor of leishmanial topoisomerase IB, exhibits antileishmanial activity, demonstrating an IC50 value of 34.81μM against L. donovani promastigotes [1].

Compound 13, a topoisomerase I inhibitor 10, selectively inhibits leishmanial topoisomerase IB and exhibits antileishmanial activity. Specifically, it demonstrates efficacy against L. donovani promastigotes with an IC50 value of 27.91 μM [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.

Topoisomerase II Inhibitor 16 (compound CT3) is a selective, orally bioavailable, and irreversible inhibitor of trypanosomal topoisomerase II, possessing the ability to penetrate the brain and stabilize double-stranded DNA-enzyme cleavage complexes. It shows promise for research into Chagas disease [1].

Topoisomerase IIα-IN-8 (compound 15) serves as a modest inhibitor of human DNA topoisomerase IIα (htIIα), exhibiting an inhibitory concentration (IC50) of 462 ± 38.0 μM [1].

Topoisomerase II inhibitor 5 (Compound E24) is a DNAtopoisomerase II inhibitor with anticancer effects.

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

Topoisomerase I/II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) . By inhibiting PI3K /Akt/mTOR signaling pathway, Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis . Topoisomerase I/II inhibitor 3 has research value in liver cancer.

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 inhibitor of topoisomerase II. Topoisomerase II inhibitor 4 has antitumour effects, blocking the cell cycle in the G2/M phase, inhibiting the proliferation of cancer cells and exhibiting cytotoxicity. It inhibits the proliferation of cancer cells and exhibits cytotoxicity.

Topoisomerase IIα-IN-3 is a DNA-inserting topoisomerase-Iiα inhibitor that blocks the cell cycle in G0/G1 phase and induces apoptosis.

Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].

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 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.

Topoisomerase I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity. It effectively inhibits 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 IIα-IN-2 (compound 5) is a DNA-binding ligands and a potent inhibitor of the topoisomerase TopoIIα. Topoisomerase IIα-IN-2 exhibits high anti-proliferative activity in human cancer cell lines. Topoisomerase IIα-IN-2 arrests the cell cycle of cancer cells in the G2/M phase and significantly induces DNA damage.

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) shows good anti-proliferative activities and arrest the cell cycle at G2/M phase. Topoisomerase II inhibitor 8 is a potent inhibitor of topoisomerase II (IC 50 = 0.52 μM) [1].

Topoisomerase I/II inhibitor 4 is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) with inhibitory effects on cell proliferation, invasion and migration, and induction of apoptosis, and can be used to study hepatocellular carcinoma.

Topoisomerase I inhibitor 2 (ZML-8) is a highly selective DNA topoisomerase I (Top1) inhibitor that inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis with anti-tumor effect [1].

Topoisomerase II inhibitor 7, a potent inhibitor of the topoisomerase II alpha subtype, exhibits an IC50 of 3.19 μM. It effectively induces cell cycle arrest and apoptosis.

Topoisomerase IV inhibitor 2 (compound 7d) is a potent inhibitor of DNA topoisomerase IV (TOPO IV), exhibiting IC50 values of 0.23 μM for TOPO IV and 0.43 μM for DNA gyrase. It also demonstrates antibacterial efficacy, with minimum inhibitory concentrations (MICs) of 0.972 μM against Staphylococcus aureus Newman and 0.608 μM against Escherichia coli ATCC8739 [1].

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.

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1].

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

Topoisomerase II inhibitor 10 is a potent inhibitor of topoisomerase II (IC50: 7.45 μM). Topoisomerase II inhibitor 10 was able to arrest the cell cycle of HepG-2 cells in the G2-M phase and induce apoptosis.

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

Topoisomerase IV inhibitor 2 (compound 5d) is a potent inhibitor of DNA topoisomerase IV (TOPO IV), exhibiting IC50 values of 0.35 μM for TOPO IV and 0.55 μM for DNA gyrase. It also demonstrates antibacterial properties, with minimum inhibitory concentrations (MICs) of 1.985 μM against Staphylococcus aureus Newman and 0.744 μM against Escherichia coli ATCC8739 [1].

Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I that traps the DNA-Top1 cleavage complex and has low cytotoxicity in non-cancerous cell lines. Research value.

Topoisomerase IIα-IN-1 (compound 2) is a DNA-binding ligands and a potent inhibitor of TopoIIα, a topoisomerase. topoisomerase IIα-IN-1 shows good anti-proliferative effects on human cancer cell lines.

Topoisomerase I/II inhibitor 2 (compound 1a) can significantly reduce the xenograft tumor growth in mice model which can be used in treating liver cancer. Topoisomerase I/II inhibitor 2 is a DNA topoisomerase I/II dual inhibitor. Topoisomerase I/II inhibitor 2 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 15 (compound 2g) serves as a potent apoptotic inducer, exhibiting heightened selectivity for head and neck tumors [1].

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

Topoisomerase II inhibitor 11 (compound 3d) is a potent inhibitor of Topoisomerase II (IC50: 2.89 μM). Topoisomerase II inhibitor 11 inhibits cell proliferation and has apoptotic activity by blocking the cell cycle in the G2/M phase.

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

Berberine hydrogen sulphate (Umbellatine Sulfate) , an alkaloid extracted from several plants, possesses antimicrobial activity against a wide variety of microorganisms including Gram-positive and Gram-negative bacteria, fungi, and protozoa.

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

Prulifloxacin (NM441) is a broad-spectrum fluoroquinolone antibiotic. It Inhibits bacterial DNA synthesis by inhibiting the activity of bacterial DNA topoisomerase II and IV.

Chloroquinoxaline sulfonamide (Chloroquinoxaline) is a topoisomerase II alpha/beta toxin with antitumor activity and immunosuppressive properties that inhibits the proliferation of B16 melanoma cells in mice, and can be used to study metastatic colorectal cancer. It can be used to study metastatic colorectal cancer.

Ciprofloxacin monohydrochloride (Bay-09867 hydrochloride) is a broad-spectrum antimicrobial carboxyfluoroquinoline.

EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity.It inhibits replication of severe acute respiratory syndrome coronavirus (SARS-CoV) in Vero 76 cells, Middle East respiratory syndrome coronavirus (MERS-CoV) in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s =0.1, 0.15 and 0.3 μM, respectively)

NU2058 (O(6)-Cyclohexylmethylguanine) is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.

Berberine chloride (Natural Yellow 18) is an alkaloid from Hydrastis canadensis L., Berberidaceae and also found in many other plants. It is relatively toxic to parenterally but has been used orally for various fungal and parasitic infections and an anti-diarrheal.

Genistein (NPI 031L) is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA TOPOISOMERASES, TYPE II), with antineoplastic and antitumor activities.

Exatecan Mesylate (DX8951f) is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC).. CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .