The presence of a trifluoromethyl rather than a methyl substituent in the bay-region greatly decreases the DNA-binding and tumour-initiating activity of the cyclopenta[alpha]phenanthren-17-ones

Carcinogenesis. 1995 Oct;16(10):2543-7. doi: 10.1093/carcin/16.10.2543.

Abstract

The increase in carcinogenicity of polycyclic aromatic compounds following bay-region methyl group substitution involves a steric component: increasing the size of the alkyl substituent decreases the carcinogenic activity of the compound. To determine whether there is also an electronic component to this effect, we synthesized a bay-region 11-trifluoromethyl analogue of 15,16-dihydrocyclopenta[alpha]phenanthren-17-one which is sterically similar but electronically very different from the 11-methyl derivative. This trifluoromethyl derivative bound to DNA in cultures of the human mammary carcinoma cell line MCF-7 to a much lower extent than the methyl-substituted compound. The trifluoromethyl derivative did not form detectable levels of DNA adducts in the epidermis of Sencar mice and was inactive as an initiator after promotion with 12-O-tetradecanoylphorbol-13-acetate for 20 weeks. In contrast, the 11-methyl derivative formed > 3 pmol adducts/mg DNA and initiated eight papillomas per mouse. These data indicate that both the steric configuration and the electronic nature of a bay-region substituent are important in determining the overall effect of the substituent on the biological activity of the molecule.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Breast Neoplasms
  • Carcinogens / metabolism*
  • Carcinogens / toxicity*
  • Cell Line
  • DNA / metabolism*
  • DNA Adducts / metabolism*
  • Epidermis / drug effects
  • Epidermis / metabolism
  • Epidermis / pathology
  • Female
  • Gonanes / metabolism*
  • Gonanes / toxicity*
  • Humans
  • Methylation
  • Mice
  • Mice, Inbred SENCAR
  • Skin Neoplasms / chemically induced*
  • Skin Neoplasms / metabolism
  • Skin Neoplasms / pathology
  • Structure-Activity Relationship
  • Tetradecanoylphorbol Acetate / toxicity
  • Time Factors
  • Tumor Cells, Cultured

Substances

  • Carcinogens
  • DNA Adducts
  • Gonanes
  • 15,16-dihydro-11-methylcyclopenta(a)phenanthren-17-one
  • DNA
  • Tetradecanoylphorbol Acetate