topoisomerases

Artemisitene 是青蒿素的氧化形式，是一种抗疟药。青蒿素前体是青蒿素生物合成的重要基础物质，包括青蒿素 B、青蒿素、青蒿酸等。

Topoisomerases ribosomes-IN-1 (compound 30f) 作为核糖体和拓扑异构酶的抑制剂，展现出对抗大环内酯类耐药细菌的有效性。该化合物能够有效抑制细菌蛋白合成 (IC50: 0.647 μM) 和 DNA 复制 (IC50: 0.218 μM)。

Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K，是抗寄生虫，抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂，也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。

Elomotecan (BN 80927 free base) 是一种有效的拓扑异构酶 I (topoisomerases I) 和 II 抑制剂。Elomotecan 是属于高喜树碱家族 (hCPT) 的喜树碱类似物。Elomotecan 能够抑制不同种类的肿瘤，且效果更好。

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.

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)) 是 Lucanthone 的生物活性代谢产物，是一种抗血吸虫病药。它是一个噻吨酮类 DNA 嵌入剂，可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。它通过直接蛋白质结合来抑制核酸生物合成并抑制嘌呤内切核酸酶1，KD 为 10 nM。

Aclacinomycin A (Aclarubicin) 是一种从加利莱链霉菌中分离出的新型蒽环类抗生素，具有抗肿瘤活性。Aclacinomycin A 是拓扑异构酶 I 和 II 的抑制剂，抑制 RNA 活性 。Aclacinomycin A 可用于研究复发性白血病和晚期恶性淋巴瘤。

Fagaronine chloride is a potent inhibitor of Topoisomerases I.

Lycobetaine (Ungeremine) 是一种潜在的抗罗克福尔青霉和黑曲霉的生物杀菌剂。它对柱状黄杆菌有很强的抗菌活性。它有效地靶向哺乳动物以及细菌I 型和II 型拓扑异构酶。它显示出强烈的乙酰胆碱酯酶抑制活性（IC(50) 值为 0.35 microM）。 它具有抗原生动物活性，在体外试验中对Trypanosoma brucei rhodesiense、T. cruzi 表现出良好的活性。

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.

Topotecan (NSC-609669) 是一种拓扑异构酶 I 抑制剂，通过抑制 DNA 拓扑异构酶起抗肿瘤作用，可用于治疗卵巢癌。

EGFR-IN-45 是一种有效的表皮生长因子受体 (EGFR) 泛抑制剂，能够作用于 EGFR (IC50: 0.4 μM) 和 CDK2 (IC50: 1.6 μM)。EGFR-IN-45 对拓扑异构酶 Topo I 和 Topo II 也具有抑制作用。EGFR-IN-45 能将癌细胞的细胞周期阻滞在 G1 前期，并诱导细胞凋亡 (apoptosis)。

Aurintricarboxylic acid (NSC-4056) 是高效的αβ-亚甲基-ATP 敏感选择性P2X1Rs 和P2X3Rs 变构拮抗剂。 它是核糖核酸酶和拓扑异构酶 II 的有效抑制剂，可阻止核酸与酶结合。

Saintopin是一种抗肿瘤抗生素，同时也是DNA拓扑异构酶I和II的抑制剂（抑制剂）。Saintopin能够诱导DNA裂解。

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 have DNA topoisomerases I and II inhibitory activity and 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.