Topoisomerase

Mitoxantrone (mitozantrone) 是一种拓扑异构酶 II (Topo II) 的抑制剂，一种蛋白激酶 C (PKC) 的抑制剂 (IC50=8.5 μM)。Mitoxantrone 具有抗肿瘤活性，可以治疗急性髓系白血病、肝细胞癌、乳腺癌等。

Topoisomerase I inhibitor 3 (Compound ZML-14) 诱导 HepG2 细胞凋亡，并在 G2/M 期阻滞细胞周期。Topoisomerase I inhibitor 3 是与拓扑异构酶 I-DNA 复合物相互作用的拓扑异构酶 I 抑制剂。

Namitecan is an effective inhibitor of topoisomerase I. It has antitumor property.

Gatifloxacin hydrochloride (AM-1155 hydrochloride) 是一种氟喹诺酮类抗生素，有广谱抗菌活性。它可抑制大肠杆菌 DNA 解旋酶 (IC50=0.109 μg/ml)和细菌 II 型拓扑异构酶(IC50=13.8 μg/ml) 。它在动物模型中，可研究细菌性结膜炎。

Etoposide Phosphate是一种选择性和可口服的topoisomerase II抑制剂和癌症化疗药品，通过DNA损伤、p53通路和细胞周期G2/M阻滞,抑制癌细胞的生长和诱导凋亡

(4-NH2)-Exatecan是一种拓扑异构酶抑制剂，具有潜在的抗癌活性，可用于合成抗体药物共轭物（ADC）。

Pixantrone (BBR 2778 (free base)) hydrochloride is a mitoxantrone analog compound that acts as a topoisomerase II inhibitor and DNA intercalator. It displays anti-tumor activity [1] [2].

Dxd (OQM5SD32BQ) 是一种有效的DNA 拓扑异构酶 I 抑制剂（IC50= 0.31 μM）。Dxd用作HER2靶向ADC 的偶联药物。

Doxorubicin（Adriamycin）是一种具有荧光性的蒽环类抗肿瘤抗生素，可抑制Topoisomerase I/II，诱导细胞凋亡和自噬，下调AMPK信号通路，常用于肿瘤化疗，并可用于诱导肾炎和心力衰竭模型。

Garenoxacin mesylate, a novel oral des-fluoro quinolone, has potent antimicrobial activity against common respiratory pathogens, including resistant strains and Gram-negative and Gram-positive bacterial infections.

CZ-48 is a DNA topoisomerase inhibitor.

Pirarubicin HCl is the hydrochloride salt form of pirarubicin, an analogue of the anthracycline antineoplastic antibiotic doxorubicin with antineoplastic activity. Pirarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair as well as RNA and protein synthesis. This agent is less cardiotoxic than doxorubicin and exhibits activity against some doxorubicin-resistant cell lines.

Topoisomerase II inhibitor 8 (化合物 22) 显示出良好的抗增殖活性，并将细胞周期阻滞在 G2/M 期。Topoisomerase II inhibitor 8是拓扑异构酶 II 的有效抑制剂 (IC 50 = 0.52 μM)。

Isosteviol ((-)-Isosteviol) 是一种常见的天然甜味剂，属于四环二萜糖苷，是甜菊糖苷通过酸催化水解产生的。它抑制 DNA 聚合酶和 DNA 拓扑异构酶，具有抗菌、抗癌和抗结核作用。

Mal-PEG8-Phe-Lys-PAB-Exatecan（化合物15）作为抗体药物偶联物（ADC）的药物连接子部分，由Mal-PEG8-Phe-Lys-PAB这一可降解连接子和毒素分子Exatecan构成。

Banoxantrone D12 (AQ4N D12) dihydrochloride is the deuterium-labeled Banoxantrone. Banoxantrone is a bioreductive agent that can be reduced to a stable, DNA-affinity compound AQ4, which is a topoisomerase II inhibitor.

The compound is a synthetic anthracycline antibiotic. It inhibits DNA topoisomerase II.

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.

Lamellarin D (Lamellarine D) 是一种从海洋无脊椎动物中分离的六环吡咯生物碱,是一种线粒体靶向型的拓扑异构酶 I 抑制剂，也是一种促凋亡剂。

BNS-22是一种DNA topoisomerase II(Topo II)抑制剂，对人的TopoIIα和TopoIIβ介导的动质体(kinetoplast)DNA十烷化的IC50值分别是2.8μM和0.42μM。BNS-22能够诱导有丝分裂异常，对人类癌细胞具有抗增殖活性。

Etoposide phosphate disodium (BMY-40481 disodium), a phosphate ester prodrug of etoposide, functions as a potent chemotherapeutic agent by selectively inhibiting topoisomerase II, hindering the re-ligation of DNA strands. It is regarded as the active equivalent of etoposide, effectively inducing cell cycle arrest, apoptosis, and autophagy in cancer cells.

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) 是一种 DNA 结合配体 (DNA-binding ligands)，也是一种拓扑异构酶 TopoIIα的有效抑制剂。Topoisomerase IIα-IN-2 对人癌症细胞株表现出较高的抗增殖活作用。Topoisomerase IIα-IN-2 能够将癌细胞的细胞周期停滞在 G2/M 期，明显诱导 DNA 损伤。

Nalidixic acid sodium salt (Baktogram) 是一种喹诺酮类抗生素，对革兰氏阳性和革兰氏阴性细菌均有效。它在较低浓度下有抑菌作用，在较高浓度下有杀菌作用。它抑制 DNA 促旋酶和拓扑异构酶IV 的亚基，并可逆地阻止易感细菌中的 DNA 复制。

Yohimbic acid是一种天然的Yohimbine的衍生物，对topoisomerase 1/2具有μM级别的弱抑制作用。

Ciprofloxacin hydrochloride monohydrate (Bay-09867 hydrochloride monohydrate) 是一种具有高效抗菌活性的氟喹诺酮类抗生素。

T-2513 hydrochloride 是拓扑异构酶 I (topoisomerase I) 的选择性抑制剂。T-2513 hydrochloride 能够共价结合拓扑异构酶 I-DNA 复合物，保持其稳定性，并能够抑制 DNA 复制和 RNA 合成，导致细胞死亡。

(±)-Evodiamine是一种发现于Evodiae fructus的生物碱和topoisomerase I抑制剂，还能抑制脂肪细胞分化和糖尿病，可以下调IGF-1/HIF-1α和IL-6/STAT。(±)-Evodiamine是NF-kB激活的抑制剂，能抑制侵袭和促进凋亡，还能抑制TNF诱导的Akt活化。

XR-5000 is a DNA topoisomerase I and II inhibitor.

Topotecan hydrochloride (NSC609699) 是一种具有抗癌活性的拓扑异构酶I 抑制剂。

Simmitecan hydrochloride 是一种喜树碱衍生物，是一种拓扑异构酶 I 抑制剂，具有抗癌活性，可用于研究是实体瘤。

Levofloxacin hydrate (Cravit hydrate) 是抗生素化合物，抑制细菌DNA 旋转酶活性。

Belotecan (CKD-602 free base) 是一种 DNA topoisomerase I 抑制剂。Belotecan 能够阻滞细胞周期，并诱导细胞凋亡。Belotecan 是一种具有抗肿瘤作用的喜树碱衍生物，能够用于研究癌症。

MC-VA-PAB-Exatecan是一种用于合成ADC的药物-连接子偶联物,含有ADC linker（MC-VA-PAB）和topoisomerase I抑制剂Exatecan，具有抗肿瘤活性。

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.

MC-GGFG-AM-(10Me-11F-Camptothecin) 是ZW251合成的Linker-Payload偶联物。ZW251是靶向人GPC3的抗体-活性分子偶联物(ADC)，包括人源化IgG1抗体、喜树碱(camptothecin)类的扑异构酶1抑制剂ZD06519及连接子（马来酰亚胺锚定和甘酰甘酰苯丙酰甘氨酸(GGFG)-氨基甲基(AM)可切割连接体）。该药物对人和食蟹猴GPC3具高亲和力，在表达GPC3的HCC细胞系中快速内化并可对GPC3阴性癌细胞进行旁观者介导杀伤。