intercalation

BMH-21, a small molecule DNA intercalator, binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and not affects phosphorylation of H2AX.

UNBS3157 is a novel naphthalimide derivative that is non-hematotoxic and exhibits significant antitumor activity through DNA intercalation and the poisoning of topoisomerase IIalpha. Unlike Amonafide, a related naphthalimide compound that showed activity in Phase II breast cancer trials but did not proceed to Phase III due to dose-limiting myelotoxicity, UNBS3157 has a maximum tolerated dose 3-4 times higher and does not cause hematotoxicity in mice at effective antitumor doses. In vivo models, including (i) L1210 mouse leukemia, (ii) MXT-HI mouse mammary adenocarcinoma, and (iii) human A549 non-small cell lung carcinoma and BxPC3 pancreatic cancer orthotopic models, demonstrate superior efficacy of UNBS3157 compared to Amonafide.

7-tert-Butylfascaplysin (7-TB) is a derivative of Fascaplysin, isolated from Fascaplysinopsis sp. It induces replication stress, leading to toxic DNA double-strand breaks and apoptosis-like cell death, exhibiting nanomolar cytotoxicity against cancer cells. Additionally, 7-tert-Butylfascaplysin demonstrates DNA intercalation activity, with an EC50 of 3.2 μM.

Antitrypanosomal agent 24 is a benzothiazole amidoxime compound with potent and selective activity against trypanosomes (IC50 = 0.92 μM). It serves as a substrate for the P-glycoprotein efflux pump and exhibits high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA via intercalation.

Dichloro(bipyridine)platinum is a potent platinum-based antitumor complex and a structural analogue of cisplatin. The incorporation of the bipyridine ligand enhances its lipophilicity and planar stacking ability. The compound interacts with DNA through covalent binding or intercalation, forming cis-Pt-DNA adducts that disrupt DNA replication and transcription. Research indicates that such complexes effectively activate pro-apoptotic signaling pathways and exhibit significant growth inhibition across various cancer cell lines, including those resistant to cisplatin. It serves as a foundational scaffold for developing next-generation metallodrugs in oncology.

Antibacterialagent 306 (Compound 8c) is a potent antibacterial agent that functions as a lactate dehydrogenase inhibitor, showing particular efficacy against Gram-positive bacteria. It has a minimum inhibitory concentration (MIC) as low as 1 μg/mL against Staphylococcus aureus. Antibacterialagent 306 disrupts cell membrane integrity, blocks DNA replication through intercalation, and induces reactive oxygen species (ROS) bursts. This compound is suitable for studying multi-drug resistant bacteria.

AT-9 is an anthraquinone-triazine derivative known for its strong DNA intercalation capability. It can interact with Topo IIA and exhibits anticancer activity against non-small cell lung cancer and cervical cancer.

Antibacterialagent 330 is an antibacterial agent that accumulates reactive oxygen species (ROS), forms DNA supramolecular complexes to block DNA replication through intercalation, and inhibits lactate dehydrogenase (LDH) to disrupt metabolism. This process leads to bacterial cell rupture and intracellular content leakage, ultimately causing bacterial death. Antibacterialagent 330 has demonstrated antibacterial activity and promoted wound healing in both Galleria mellonella larvae and mouse wound infection models. It is suitable for research on bacterial infections.

MitoNeoD is a novel mitochondria-targeted O2 (⋅−) probe that can be used in vivo. It prevents DNA intercalation. MitoNeoD incorporates a carbon-deuterium bond, and enhances O2 (⋅−) selectivity.

YO-Pro 1, a cyanine dye consisting of benzoxazole and quinoline rings connected by a linker, is almost nonfluorescent in water, but its fluorescence is greatly enhanced after intercalation in double-stranded DNA, forming the basis of DNA concentration assays. Ex/Em (bound DNA) = 491/509 nm. YO-Pro 1 can be used to identify apoptotic cells.

Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNA ligase A at concentrations of 50 uM. At the chemical screening was found that pinafide inhibited B-Myb transcriptional activity in luciferase assays. The cross placental-barrier studies showed that 3H-pinafide was present in the 14-day fetuses.

Amikhellin HCl, an antimitotic drug, is a synthetic water-soluble derivative of khellin, an alkaloid extracted from seeds of Ammi Visnaga. Amikhellin has been used so far mostly as a vasodiator. Amikhellin binds to double-stranded DNA by an intercalation process. It inhibits the DNA-polymerase from murine sarcoma leukemia virus.

Cyclopentenylcytosine (CPC), a nucleoside analog, effectively inhibits CTP synthetase, leading to reduced levels of cytidine triphosphate (CTP) and deoxycytidine triphosphate (dCTP) in leukemic cells. Furthermore, it enhances the phosphorylation of 1-β-D-arabinorubosylmannosylcytidine (araC) and increases its DNA intercalation activity. In the human T lymphocyte line MOLT-3, cyclopentenylcytosine triggers apoptosis and necrosis in a dose (50-300 nM) and time (8-16 h) dependent manner. When used in conjunction with araC, cyclopentenylcytosine augments the induction of both apoptosis and necrosis, amplifying its cytotoxic effects on T lymphoblasts.

Iron (III) sulfate solution serves as a sodium ion intercalation agent and a sodium storage material. It can be utilized in studies related to the development of sodium-ion battery electrodes.