5F-DF-203-L-LYSINAMIDE (Phortress) is an experimental antitumor agent with potent and selective activity against human-derived carcinomas of breast, ovarian and renal origin. The mechanism of action of Phortress is distinct from all classes of chemotherapeutic agents currently in the clinic, and involves metabolic activation by cytochrome P450 (CYP) 1A1 to electrophilic species, which generate DNA adducts in sensitive tumors only. Phortress is in phase I clinical trials for the treatment of solid tumours. The compound was co-developed by Pharminox, University of Nottingham and Cancer Research UK.

Chelerythrine is a kind of benzo[c] phenanthridine alkaloids, which is widely found in plant of Fumariaceae, Papaveraceae, Ranunculaceae and Rutaceae families. Chelerythrine is a potent and specific inhibitor of protein kinase C. In addition chelerythrine inhibits pro-survival protein Bcl(XL) thereby inducing apoptosis. It exerts antitumor properties.

Sterigmatocystin is a mutagenic and carcinogenic mycotoxin initially produced by species of Aspergillus. Sterigmatocystin is a precursor of aflatoxin B1. In vitro, Sterigmatocystin activates ATM, p53, and Chk2 and damages DNA, inducing G2 phase cell cycle arrest; this mechanism may also involve PI3K/Akt/mTOR signaling. In vivo, chronic administration of sterigmatocystin decreases levels of glutathione, ascorbic acid, and α-tocopherol and increases levels of ROS, increasing lipid peroxidation.

UNBS5162 is a naphthalimide that binds to DNA by intercalation and suppresses CXCL chemokine elaboration. In vivo and in vitro studies demonstrated potent antineoplastic properties of the compound. The phase 1 dose-escalation trial demonstrated that despite pre-clinical data suggesting low risk of QTc prolongation with UNBS5162 administration, there was a statistically significant relationship noted in study patients. The magnitude of QTc prolongation at the highest doses warranted the study drug to be terminated.

The DOTAP (N-[1-(2,3-Dioleoyloxy)propyl]-N,N,N-trimethylammonium methyl-sulfate) is a liposomal transfection reagent suitable for transient and stable transfection of mammalian cell lines with DNA (plasmids, bacmids) and modified nucleic acids (antisense oligonucleotides). Mixing DOTAP with DNA results in spontaneously formed stable complexes. These complexes can be added directly to the tissue culture medium. This method avoiding the cytotoxic effects commonly encountered with lipofection or others transfection methods. The recently published article described the ability of R-DOTAP stabilized microparticles (MP) to act as a carrier platform for antigens e.g. for cancer vaccination. It was investigated whether or not a combination of R-DOTAP and PLGA leads to a boosted adjuvant effect in dendritic cell maturation.

Bisbenzimide ethoxide is a fluorescent nucleic acid stain useful for DNA labeling in fluorescence microscopy and flow cytometry. It appears to bind to AT-rich regions containing at least four such basepairs. Bisbenzimide ethoxide seems to bind relatively poorly to nucleotide sequences containing the alternating step TpA. Bisbenzimide ethoxide induced apoptosis in the HL-60 cells in a time- and dose-dependent manner. Endogenous nuclear topoisomerase I activity in HL-60 cells was inhibited by treatment with Bisbenzimide ethoxide.

COPPER(II) 4-OXOPENT-2-EN-2-OLATE (Copper(II) acetylacetonate [Cu(acac)2]) is a soluble copper catalyst that has been widely employed in many types of reactions. It is a powerful reagent in organic synthesis. Anticancer properties of Copper(II) acetylacetonate complex was found by treating different cancer cell lines. The TUNEL assay showed a strong positivity in the C6 cells treated with Cu(acac)2 and this indicates that the Cu compounds initiated cell death by DNA fragmentation.

CUPRIC ETHYLENEDIAMINE is a purple liquid with an ammoniacal odor. It is used to dissolve cellulose products to give a cuprammonium-type solution. Superoxide ion is generated as an intermediate at the first reaction step between CUPRIC ETHYLENEDIAMINE and H2O2. DNA strand scission may be caused by hydroxyl radicals generated from the reaction of CUPRIC ETHYLENEDIAMINE with biological reductants under aerobic conditions. Since ascorbic acid, is present in living cells, CUPRIC ETHYLENEDIAMINE may be capable of initiating DNA damage in the presence of this reductant. Inhalation of vapor CUPRIC ETHYLENEDIAMINE irritates mucous membrane and may cause asthma. Liquid causes severe irritation of eyes and possible corneal injury. Contact with skin causes irritation. Ingestion causes irritation of mouth and stomach.