intercalator

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。

Pixantrone dimaleate (Pixantrone Maleate) 是一种拓扑异构酶 II 的抑制剂和 DNA 嵌入剂，是一种实验性抗肿瘤药物。

LMP744 is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.

LMP744 hydrochloride (NSC-706744 hydrochloride) 是一种是拓扑异构酶 1 抑制剂，显示出抗肿瘤的活性。

BMH-21 是一种小分子 DNA 嵌入剂，可结合核糖体 DNA 并抑制 RNA 聚合酶 I (Pol I) 转录，具有抗癌活性。

AcLysValCit-PABC-DMAE-SW-163D is a drug-linker conjugate for antibody-drug conjugates (ADCs), featuring a natural bis-intercalator, SW-163D, attached through an AcLysValCitPABC-DMAE linker[1].

TopoisomeraseII inhibitor 19 (compound 5h) 是一种同时具有 DNA 嵌入能力的拓扑异构酶 II (TopoisomeraseII) 抑制剂，其 IC50 值为 0.34 μM。此化合物还能够在 ctDNA 中诱导损伤。

NSC 727357 是一种具有抗肿瘤活性的 DNA 嵌入剂和拓扑异构酶 (topoisomerase) 抑制剂。它能够抑制细胞增殖并诱导 G1 期阻滞。NSC 727357 可应用于包括黑色素瘤在内的癌症研究。

BPTQ is a typical intercalator of DNA that acts by inducing a dose-dependent inhibitory effect on the proliferation of cancer cells by arresting cells at the S and G2/M phase.

Bisnafide is a Naphthalimide Analogue that acts as a DNA intercalator and topo II inhibitor. It is also an antiangiogenic agent that can normalize tumor vessels and promote the delivery of cytotoxic agents to tumor sites.

Crisnatol, a potent and selective DNA intercalator, has potential anticancer activity.

BePI can be a specific intercalator of both double and triple-helical DNA.

Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively). 1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)

Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg/ml, respectively). It is cytotoxic to B16/F10 and Moser cells (IC50s = 0.0008 and 0.04 μg/ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).

Amustaline (S-303) dihydrochloride is a nucleic acid-targeted alkylator recognized for its efficacy as a pathogen inactivation agent in blood components containing red blood cells. This compound comprises three key elements: an acridine anchor (a non-covalently bonding intercalator targeting nucleic acids), an effector (a bis-alkylator group that interacts with nucleophiles), and a linker (a flexible carbon chain with a labile ester bond, hydrolyzing at neutral pH to non-reactive products).

Bisantrene (CL-216942; NSC 337766) is a topoisomerase II poison and DNA intercalator. It can be used as a Rac1 inhibitor or model compound to study P-glycoprotein-mediated multi-drug resistance (MDR1). Bisantrene inserts and disrupts the configuration of

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。

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].

Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase.

Bisnafide is a Naphthalimide Analogue that acts as DNA intercalator and topo II inhibitor. It is also an antiangiogenic agent. Antiangiogenic agents can normalize tumor vessels and promote the delivery of cytotoxic agents to tumor sites.

Crisnatol (BWA770U) 为口服有效的抗癌剂，属于芳甲基氨基丙二醇类 DNA 插入剂。该化合物在体外对人类乳腺癌细胞表现出细胞毒性，而对正常人类皮肤成纤维细胞则无显著影响。