4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone or nicotine-derived nitrosamine ketone (NNK) is a tobacco-specific nitrosamine. NNK is considered to be a carcinogen. NNK induces deleterious mutations in oncogenes and tumor suppression genes by forming DNA adducts, which could be considered as tumor initiation. Meanwhile, the binding of NNK to the nicotinic acetylcholine receptor promotes tumor growth by enhancing and deregulating cell proliferation, survival, migration, and invasion, thereby creating a microenvironment for tumor growth.

PET imaging using 2-[11C]thymidine (dThd) was developed as a measure of tumor proliferation and cancer response to treatment. The drug was tested on patients with brain tumors. A PET image is a result of the metabolic processes for delivery, uptake, and retention in DNA by the tumor and degradative metabolism in the whole patient. 2-[11C]Thymidine is metabolized to [C11]CO2, which rapidly crosses the blood-brain barrier and distributes throughout the brain. 2-[11C]Thymidine itself is poorly transported by the blood-brain barrier, however, it may intercalate into DNA.

Azomycin (2-Nitroimidazole) is a natural antimicrobial antibiotic produced by a strain of Nocardia mesenterica, that have been used to combat anaerobic bacterial and parasitic infections. Azomycin and other 2’-nitroimidazoles show anti-ischemic and anti-inflammatory pharmacological properties. Azomycin is cytotoxic and change drug-metabolizing cytochrome P450, NADPH dependent reductase enzymes and cause depletion of tissue oxygen pressure. Azomycin is a prodrug. Unionized Azomycin is selective for anaerobic bacteria due to their ability to intracellularly reduce Azomycin to its active form. This reduced Azomycin then covalently binds to DNA, disrupt its helical structure, inhibiting bacterial nucleic acid synthesis and resulting in bacterial cell death.

Gene therapy is expected to treat various incurable diseases including viral infections, autoimmune disorders, and cancers. Complexes of cationic liposomes with DNA are promising tools to deliver genetic information into cells for gene therapy and vaccines. Electrostatic interaction is thought to be the major force in lipid–DNA interaction, while lipid-base binding and the stability of cationic lipid–DNA complexes have been the subject of more debate in recent years. 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) forms heterogeneous liposomes with cationic lipids, which are used as delivery vehicles for therapeutic agents. DOPE is an essential component of cationic liposomes designed to deliver DNA into gliosarcoma and kidney cell lines (gene therapy). The order of stability of lipid–DNA complexation is DOTAP>DDAB>DOPE>Chol. Recently was discovered Lip-DOPE-MPL-GP2 formulation could be a promising vaccine and a therapeutic delivery system against HER2 positive cancers and merited further investigation.

The gluconate formulation of amsacrine (AMSA) has better water solubility then DMA formulation. It was thus developed and investigated to determine if it would be less cardiotoxic than the widely used N,N-dimethylacetamide (DMA) formulation. Amsacrine gluconate is the anticancer agent, which was tested against refractory leukemia. Moreover, their cytotoxic activity was demonstrated in the in vitro studies on 48 specimens of 9 histologically different types of human malignancy. The use of the gluconate formulation of AMSA, which contains no dimethylacetamide, has been associated with three cases of cardiomyopathy. Also, paresthesia was found in one patient among 26 treated with AMSA gluconate. This preparation has no apparent advantage when compared with amsacrine lactate.

Tubercidin, an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.