Topoisomerase

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

Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) 是一种经常使用在极性溶液中具有高溶解度的胆固醇类似物 ，具有保肝、抗癌和抑制肿瘤生长的作用。Cholesteryl Hemisuccinate 抑制对乙酰氨基酚 的肝毒性，并防止 AAP 诱导的肝细胞凋亡 和坏死 。Cholesteryl Hemisuccinate 抑制 DNA 聚合酶 和 DNA 拓扑异构酶 ，从而抑制 DNA 复制和修复以及细胞分裂。

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.

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 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。

Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) 为一种基于 exatecan 的衍生物，常见于药物缀合物的有效载体中。该化合物在抑制多种肿瘤细胞系方面展示出优异的活性。

Anticanceragent 215 (1)，一种喜树碱类化合物，展现了对MCF-7与MDA-MB-231细胞的显著抑制作用，其IC50值分别是5.2 nM和8.2 nM。

Anticanceragent 216 (34A) 是一种喜树碱衍生物，对 MCF-7 细胞和 MDA-MB-231 细胞的 IC50值分别为 9.6 nM 和 11.6 nM。

TopoisomeraseI inhibitor 17 (Compound 7h) 是一种TopoisomeraseI (Top1)抑制剂，可减少 DDX5，并逆转 DDX5 对 Top1 活性的锁定，诱导 Top1 介导的 DNA 损伤并促进活性氧 (ROS)产生。它通过减少抗凋亡蛋白XIAP、Bcl-2、Survivin并增加促凋亡蛋白Bax、γH2AX，诱导细胞凋亡。此外，它阻止 G2/M 检查点的进展，导致细胞周期阻滞。该化合物显著抑制结直肠癌细胞的集落形成和迁移能力，且有效降低人类 PDX 肿瘤模型小鼠的肿瘤大小。

Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. Atiratecan does not inhibit acetylch

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。

Topobexin (Topobexin 9) 是一种高度选择性的TOP2B抑制剂。它在体外优先抑制TOP2B，并将其固定在DNA上。Topobexin 对心肌细胞具有显著的保护作用，防止DAU引起的损伤。在兔模型中，它可预防由蒽环类药物引起的心脏毒性和DAU诱导的左心室收缩功能下降。

Epolactaene is a neuritogenic compound in human neuroblastoma cells which selectively inhibit the activities of mammalian DNA polymerases and human DNA topoisomerase II.

SelB-1 是一种针对拓扑异构酶 I/II (Topoisomerase I/II) 的双重抑制剂，展现出在前列腺癌和结肠癌研究中的抗癌活性。此外，SelB-1 还可以诱导自噬 (autophagy) 基因的表达和脂质过氧化，并能有效降低GSH水平。

(R)-Sitafloxacin (DU-6857) 是 Sitafloxacin (DU-6859a) 的一个对映异构体，并且是一种拓扑异构酶抑制剂，其对 DNA 旋转酶的 IC50 为 0.18 μg/mL。

Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) 是一种用于ADC（抗体偶联药物）的药物-连接体偶联物。它由DNA拓扑异构酶 I 的强效抑制剂Exatecan和连接子Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB构成，用于制备抗体偶联物AZD0516。

Melicopidine (NSC 34757) 是一种DNA topoisomerase抑制剂，同时也是从Medicosma subsessilis树皮中发现的吖啶酮类生物碱。它通过结合DNA或抑制相关酶活性来展现潜在的抗肿瘤效果。

Topo II/HDAC-IN-2 (8d) 是一种具有针对Topo II和HDAC的双重抑制活性的化合物，能有效诱导细胞凋亡。

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。

CP 67015 has an inhibitory effect on the function of topoisomerase, and is a direct mutagen in mammalian cells, which has effects on gene and chromosome levels.

A 9387 is an inhibitor of resolvase protein.

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)。

CZ-48 is a DNA topoisomerase inhibitor.

TLC 388, a DNA topoisomerase I inhibitor, is used potentially for the treatment of Renal carcinoma and Hepatocellular carcinoma

Pixantrone 具有抗肿瘤活性。它是一种 DNA 嵌入剂和拓扑异构酶 II 抑制剂。

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.

Thaspine acetate is a potent topoisomerase IB inhibitor. Taspine downregulates VEGF expression and inhibits proliferation of vascular endothelial cells through PI3 kinase and MAP kinase signaling pathways.

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].

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-hydroxyellipticine is a potent cytotoxic and antitumor agent. 9-hydroxyellipticine is a 9-hydroxy derivative of ellipticine.

BO 2367, a topoisomerase inhibitor, is used to suppress the growth of tumor .

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。

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。

Moflomycin is an anthracycline derivative. It exhibits a higher antileukemic activity compared to other anthracyclines.

tau-0N4R-IN-1（Compound 6T）作为一种穿透脑屏障的抑制剂，能够抑制tau 0N4R、2N3R及2N4R的纤维化。该化合物具有显著的抗播种效应，在体外能够剂量依赖地减少α-syn的寡聚，并阻止α-syn包涵体的形成。在小鼠微粒体中表现出稳定性，并能减少AD患者脑组织中的Aβ斑块。此外，tau-0N4R-IN-1在小鼠体内展示出优良的药代动力学特性。

Idarubicin 是一种有效的、具有口服活性的蒽环类抗白血病剂。Idarubicin 抑制拓扑异构酶 II，干扰 DNA 复制和 RNA 转录。Idarubicin 可诱导 DNA 损伤。Idarubicin 抑制 DNA 合成和 c-myc 表达。Idarubicin 还抑制细菌和酵母菌的生长。