topoisomerases

Topoisomerases ribosomes-IN-1 (compound 30f) serves as an inhibitor targeting both ribosomes and topoisomerases, specifically exhibiting inhibitory actions against constitutively macrolide-resistant bacteria. This compound effectively suppresses bacterial protein synthesis (IC 50 : 0.647 μM) and hampers DNA replication (IC 50 : 0.218 μM).

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan is able to inhibit different types of tumors with better efficacy.

Finafloxacin, a fluoroquinolone antimicrobial agent from a new 8-cyano subclass, is most effective in slightly acidic environments (pH 5.0-6.0), a condition where other fluoroquinolones typically reduce in activity. It selectively targets bacterial type II topoisomerases, such as DNA gyrase and DNA topoisomerase IV, making it suitable for treating serious bacterial infections particularly in acidic contexts, including urinary tract infections (UTIs) and Helicobacter pylori infections.

Topotecan (NSC-609669) is a Topoisomerase I inhibitor,and is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

1. Lycobetaine (Ungeremine) is a potential biofungicide against Penicillium roqueforti and Aspergillus niger.2. Lycobetaine have strong antibacterial activity against Flavobacterium columnare . 3. Lycobetaine effectively targets mammalian as well as bacterial type I and type II topoisomerases.4. Lycobetaine shows strong acetylcholinesterase inhibitory activity(IC(50) value of 0.35 microM). 5. Lycobetaine has antiprotozoal activity, it shows good activity in in vitro assays against Trypanosoma brucei rhodesiense, T. cruzi.

Zabofloxacin is a potent and seletive bacterial type II and IV topoisomerases inhibitor, and has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.

Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

Artemisitene is the oxidized form of Artemisinin and is an antimalarial agent. Artemisinin precursors are the important basic substances for biosynthesis of Artemisinin, including Artemisinin B, Artemisitene, Artemisinic acid, etc.

Aclacinomycin A (Aclarubicin) is a novel anthracycline antibiotic isolated from Streptomyces galilei with antitumor activity.Aclacinomycin A is an inhibitor of topoisomerases I and II and inhibits RNA activity.Aclacinomycin A has been used in the study of relapsed leukemia and advanced malignant lymphomas.

Fagaronine chloride is a potent inhibitor of Topoisomerases I.

Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition of both topoisomerases I and II, initiating DNA cleavage and apoptosis. Becatecarin, alone or in combination with other compounds, has anti-cancer as well as myelosuppressive effects in vivo. It is also a transport substrate of the ATP-binding cassette (ABC) transporter ABCG2.

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA ethyl ester is a neutral, more lipid soluble form of the free acid.

Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA methyl ester is a neutral, more lipid soluble form of the free acid.

Elomotecan hydrochloride (BN 80927), a camptothecin analog from the homocamptothecin family (hCPT), is a highly potent inhibitor of both topoisomerases I and II. It demonstrates superior efficacy in reducing the proliferation of various tumor cells compared to other reference anticancer drugs targeting these topoisomerases.

EGFR-IN-45 is a potent pan-inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.4 μM and also targets CDK2 with an IC50 of 1.6 μM. It inhibits topoisomerases Topo I and Topo II, blocks the cancer cell cycle in the pre-G1 phase, and induces apoptosis.

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

Saintopin is an antitumor antibiotic and an inhibitor of DNA topoisomerases I and II, which induces DNA cleavage [1] [2].

Ganoderiol F has anti-inflammatory, cytotoxic and anti-HIV activity, it inhibits activity of topoisomerases in vitro, and it inhibits human immunodeficiency virus-1 protease with IC(50) values of 20-40 microM. It induced HO-1 expression, activation of the mitogen-activated protein kinase EKR and up-regulation of cyclin-dependent kinase inhibitor p16 and suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) production.

1,4-Dihydroxy-2-carbomethoxy-3-prenylnaphthalene-1-O-beta-glucopyranoside may exhibit inhibitory activity against DNA topoisomerases I and II and demonstrate cytotoxicity.

Ganoderic acid X is a potential Mdm2 inhibitor(K(i) = 16nM). It is a potential anticancer drug, inhibits topoisomerases and induces apoptosis of cancer cells.