Carcinogenic, activity properties

The carcinogenic properties of tricycloquinazoline (60) were studied in detail because of its possible formation from anthranilic acid derivatives in nature. It possessed stronger carcinogenic activity toward mice (72%) than rats (27%). Its action resembled that of embedded plastic materials, because it was recovered unmetabolized. ... 

In addition to influencing hydrocarbon metabolite-DNA reactions, the physical binding properties of hydrocarbon metabolites covalently bound to DNA may also be important to carcinogenic activity. The covalent binding of ultimate carcinogens derived from BP and DMBA to DNA produces adducts with tt binding properties similar to those of naturally occurring nucleotides. These adducts... 

Banner et al., (21) found that selenium did not influence the acute alterations induced by 2-acetylaminofluorene or methylazoxymethanol and suggested that the anticarcinogenic properties of selenium were due to a mechanism other than an interference with carcinogen activation and interaction with cellular macromolecules. 

Ethidium bromide is a common fluorescent stain for nucleic acids, ft is reported to have significant anti-tumor and anti-viral properties. However, its potential applications in human therapy are prevented, due to its mutagenic and carcinogenic activities in model organisms. 

Lacassagne A, Buu-Hoi NP, Daudel R, Zajdela F (1956) The relation between carcinogenic activity and the physical and chemical properties of angular benzacridines. Adv Cancer Res 4 315-369... 

In classical structure-activity studies, most of the attempts concentrated on correlating the activity with one of the molecular properties— e.g., the carcinogenic activity of polynuclear aromatic compounds with their electronic structure (18, 19), the narcotic activity with lipophilicity 20, 21), the insecticidal activity of cyclodienes with their three-dimensional molecular silhouette 22), etc. Sometimes the activity correlated well with only one of the molecuar parameters. In our approach these are special cases where other physicochemical properties do not play critical roles in determining the variation in the activity within a set of congeners so that the coefficients defining these other properties are zero. 

The relationship between carcinogenic activity and chemical properties is far from clear, but the possibility of uncovering this relationship has inspired a tremendous amount of research in the fields of synthesis and of structure and reactivity. 

Pullman B, Pullman A. Electron-donor or electron-acceptor properties and carcinogenic activity of organic molecules. Nature 1963 199 467-9. 

Forty-eight derivatives of berberine-type alkaloids were examined for their inhibition activity against the induction of mouse ear edema via application of 12-O-tetradecanoylphorbol-13-acetate (TPA). Berberrubine chloride displayed inhibitory effects (ED50 1.3 pmol/ear 52% inhibition). Berberine derivatives had stronger inhibitory activity than palmatine derivatives. Since berberine and some of its derivatives are present in Chinese traditional drugs, which are used in combined Kampo prescriptions, it is important to determine if such alkaloids possess carcinogenic inhibiting properties [221]. 

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