Topoisomerase

Besifloxacin Hydrochloride (BOL-303224-A) 是一种氟喹诺酮类抗生素。

Coralyne chloride 是一种具有强抗癌活性的原小檗碱。它可用于制备 Coralyne 衍生物，是一种基于荧光 DNA 的分子整流剂，通过位点特异性插入构建成 DNA 双链体。它可作为一种拓扑异构酶 I 毒性分子，诱导拓扑异构酶 I 介导 DNA 裂解。

DRF-1042 HCl 是一种具有口服活性的喜树碱类似物，具有抗肿瘤活性，抑制 DNA 拓扑异构酶 I，可用于研究难治性实体瘤。

Norfloxacin (MK-0366) 是广谱抗生素，能通过结合DNA 旋转酶抑制革兰氏阳性和阴性菌。

Ciprofloxacin monohydrochloride (Bay-09867 hydrochloride) 是一种高抗菌活性的氟喹诺酮类抗生素。

Merbarone 是一种Ⅱ型 DNA 拓扑异构酶抑制剂，可通过阻断 DNA 切割抑制人拓扑异构酶 IIα 的催化活性，继而诱导半胱天冬酶激活的 DNase 激活以及染色体 DNA 环从核基质中的切除。Merbarone 通过激活 ICE/CED-3 样蛋白酶在 CEM 细胞中触发细胞凋亡，是研究 DNA 损伤应答与细胞凋亡通路的机制性工具化合物。

WJ35435 is a histone deacetylase and topoisomerase I dual inhibitor.

Amrubicin, also known as SM-5887, is an anthracycline used in the treatment of lung cancer. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell growth inhibition and cell death. This agent has demonstrated a higher level of anti-tumor activity than conventional anthracycline drugs without exhibiting any indication of the cumulative cardiac toxicity common to this class of compounds. It is marketed in Japan since 2002 by Sumitomo Pharmaceuticals.

Topoisomerase IV inhibitor 2(compound 5d)是一种有效的Topo IV抑制剂，对Topo IV和DNA促旋酶的IC50分别为0.35 μM和0.55 μM，具有抗菌活性。

CP 67804 enhances topoisomerase II-mediated DNA cleaving.

TopoisomeraseI/II inhibitor 8 (Compound Ru7) 是一种双催化抑制剂，能够损伤DNA并激活PARP-1，随后激活RIPK1、RIPK3和MLKL，从而引发坏死性凋亡 (necroptosis)。此化合物展现出显著的抗癌活性，通过坏死性凋亡靶向癌细胞的细胞核，在克服癌症耐药性上具备巨大临床潜力。

Tryprostatin A is an inhibitor of breast cancer resistance protein and, along with tryprostatin B, is an indole alkaloid-based fungal product that inhibits the mammalian cell cycle at the G2/M phase.

Topoisomerase inhibitor6 (Compound REDX05931) 是一种双重不可逆的DNA gyrase和topoisomeraseIV抑制剂，对耐氟喹诺酮类的S. aureus的MIC为0.06 μg/mL。此化合物通过阻断DNA链断裂-重接过程引起致命的DNA损伤，有潜力用于研究革兰氏阳性菌感染，如S. aureus和S. pneumoniae。

Edotecarin is a potent topoisomerase I inhibitor. It can decrease single-strand DNA cleavage (IC50: 50 nM).

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。

3,6-Diamino-9(10H)-acridone 是拓扑异构酶的抑制剂。

Lurtotecan dihydrochloride is an antineoplastic (DNA Topoisomerase I Inhibitor)

Fostriecin (free base) is an inhibitor of the serine/threonine protein phosphatases 2A (PP2A) and 4 (PP4) (IC50s = 3.2 and 3 nM, respectively). It less effectively inhibits topoisomerase II and PP1 (IC50s = 40 and 131 μM, respectively) and does not inhibit PP2B. Through its effects on protein phosphatases, fostriecin increases the level of histone H3 phosphorylation and may alter epigenetic regulation of cell proliferation. On a related note, fostriecin was first identified as an antitumor antibiotic.

9-Hydroxyellipticine hydrochloride 是 Topo II 和 RyR 的抑制剂，具有抗肿瘤、抗氧化、抗心血管和抗白血病活性，抑制角叉菜胶诱导的水肿，可用于研究神经系统疾病和心血管疾病。

Garenoxacin (BMS284756) 是一种新型的口服 des-fluoro(6) 喹诺酮，有抗菌活性，可抑制呼吸道病原体。

TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2].

Topoisomerase I inhibitor 6 (Compound 3) 是一种 Topoisomerase I 的有效抑制剂，可以捕获 DNA-Top1 裂解复合物，在非癌细胞系中具有较小的细胞毒性。Topoisomerase I inhibitor 6 对癌症疾病表现出潜在的研究价值。

Anticancer agent 76 (Compound CT2-3) 是一种能够明显抑制人 NSCLC 细胞增殖、诱导细胞周期阻滞、ROS 生成和细胞凋亡（apoptosis）的抗癌剂。

Gly-7-MAD-MDCPT 是一种抗癌剂。Gly-7-MAD-MDCPT 是一种喜树碱 (Camptothecin) 化合物，对多种癌细胞有细胞毒性，IC50为 10-1000 nM。

10NH2-11F-Camptothecin TFA 是一种 Camptothecin 类似物，适用于作为 ADC 细胞毒素用于合成抗体药物偶联物 (ADC)。10NH2-11F-Camptothecin TFA 展现出抗癌作用 (WO2022246576A1; compound 140)。

(1-OH)-Exatecan 是一类喹啉环化合物，表现出显著的抗增殖活性，适用于癌症研究。

Makaluvamine A comes from the fruiting bodies of Didymium bahiense that act as active anti-cancer agents and DNA topo II inhibitors.

AZD-5099 is a DNA gyrase modulator potentially for the treatment of bacterial infection.

Lomefloxacin (SC47111A) 是一种广谱喹诺酮类抗生素，具有抗菌活性。它可研究支气管炎、尿路感染、结膜炎、外耳炎和中耳炎。

TAK1 inhibitor 是一种抑制剂，对MCF-7、A549 、DU-145 、MDA MB-231有抑制作用，IC50分别为 0.021、0.14、0.064 、0.19 。化合物13 具有较好的抑菌活性,麦克风范围为93.7 ~ 46.9μg / mL,麦克风范围为7.8 ~ 5.8μg / mL。

Anticancer agent 218 (P136) 是一种属于喜树碱类的化合物，具有显著的抗癌活性。

Topoisomerase I inhibitor 11 effectively inhibits Topoisomerase I and has the capability to bind to BTK [1].

Topoisomerase inhibitor2(18C)为针对细菌拓扑异构酶的抑制剂，展现出对多重耐药革兰氏阴性菌的强效广谱活性。

Top/HDAC-IN-3（Compound 31），作为一种口服活性的Topoisomerase和HDAC双重抑制剂，通过上调活性氧（ROS）水平引发DNA损伤，有效抑制癌细胞的克隆形成与迁移，同时诱导癌细胞凋亡（Apoptosis）及细胞周期阻滞。在NSCLC模型中，Top/HDAC-IN-3的抗肿瘤效果显著，其抗肿瘤效率（TGI = 77.5%，100 mg/kg）显著优于HDAC抑制剂SAHA及SAHA与拓扑异构酶抑制剂伊立替康的组合疗法。

Mal-VC-PAB-DMEA-PNU-159682 是一种结合于 ADC 的药物-连接体结合物，通过溶酶体可裂解的二肽 Mc-VC-PAB 将抗拓扑异构酶 II 抑制剂 PNU-159682 进行连接，展现出强效的抗肿瘤活性。该化合物可用于合成 Anti-CD22-NMS249。

KT32 (10c) 是一种同时抑制HDAC和Topo IIα的高效化合物，通过诱导细胞凋亡来促使细胞死亡。