topo

1,4-Naphthoquinone (P-Naphthoquinone) was used as a potential inhibitor of monoamine oxidase and DNA topoisomerase activities[2]. It was also used to inhibit the acetyltransferase activity[1].

Epirubicin hydrochloride (Pharmorubicin) is an adriamycin derivative, a topoisomerase (Topo) inhibitor, and a Forkhead box protein p3 (Foxp3) inhibitor. Epirubicin hydrochloride has antitumor activity.

Topixantrone 2HCl is a DNA topoisomerase inhibitor with antitumor activity for the study of gastric and prostate cancer.

Alalevonadifloxacin is a DNA gyrase and DNA topoisomerase inhibitor and a novel antibacterial compound of the quinolone class targeting MRSa. Alalevonadifloxacin is potentially useful in the treatment of bacterial Gram-positive, Gram-negative and anaerobic infections.

Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) is a highly soluble cholesterol analogue often used in polar solutions for its hepatoprotective, anticancer and tumour growth inhibiting properties. Cholesteryl Hemisuccinate inhibits the hepatotoxicity of acetaminophen and prevents AAP-induced apoptosis and necrosis in hepatocytes. Cholesteryl Hemisuccinate inhibits DNA polymerase and DNA topoisomerase, thereby inhibiting DNA replication and repair as well as cell division.

DNA gyrase Topo IV-IN-1 (Compound 27) is an inhibitor of DNA gyrase and topoisomerase IV with antibacterial properties. It exhibits IC50 values of 11 and 17 nM against the DNA gyrase of Escherichia coli and methicillin-resistant Staphylococcus aureus, respectively, and IC50 values of 83 and 21 nM against topoisomerase IV of the same organisms. DNA gyrase Topo IV-IN-1 is applicable in anti-infective research.

Topo I II-IN-1 (compound 7t) is an effective dual inhibitor of Topo I and Topo II. It exhibits significant cytotoxicity against the MCF-7 breast cancer cell line, with an IC50 value of 7.45 μM.

Topo I II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K Akt mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.

Topo I COX-2-IN-1 (1H-30) is a potent Topo I COX-2 inhibitor with IC50 values of 0.24 μM for COX-2 and 4.42 μM for Topo I. It induces apoptosis and inhibits cancer cell migration, demonstrating anti-cancer activity.

Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor that exhibits antitumor activity, DNA intercalative capability, and can induce cell apoptosis.

Topo I COX-2-IN-2 (Compound W10) is a potent dual inhibitor of Topo I (IC50: 0.90 μM) and COX-2 (IC50: 2.31 μM), inducing apoptosis in cancer cells via the mitochondrial pathway.

Topo II HDAC-IN-1 (7d) demonstrates potent dual inhibitory effects on Topo II and HDAC, while Topo II HDAC-IN-1 (8d) effectively induces apoptosis [1].

Topo II HDAC-IN-2 (8d) demonstrates remarkable dual inhibitory effects on Topo II and HDAC, and also induces apoptosis [1].

Datopotamab deruxtecan (DS-1062) is a trophoblast cell surface antigen 2 (TROP2)-targeted antibody-drug conjugate (ADC) with antitumor activity. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

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.

Topotecan hydrochloride (NSC609699) is an antineoplastic agent used to treat ovarian cancer.

Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride) is a substrate for affinity chromatography of heme-binding proteins.

Meta-Topolin (m-Topolin) , a highly active aromatic cytokinin from poplar leaves

Tin-protoporphyrin IX dichloride (SnPPIX dichloride) is an HO-1) inhibitor with antiviral activity that inhibits dengue and yellow fever viruses.

Hematoporphyrin is a substrate for affinity chromatography of heme-binding proteins.

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 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.

TOPOI PARP-1-IN-2 (compound 6c) serves as a dual inhibitor targeting both PARP-1 and topoisomerase 1 (TOPO-1), with IC50 values of 32.2 nM and 46.2 nM, respectively. This compound exhibits greater selectivity for PARP-1 over PARP-2. Additionally, TOPOI PARP-1-IN-2 disrupts the S phase of the cell cycle and induces apoptosis in the NCI-60 cancer cell lines.

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].