Response of transplantable tumors in mice and of macromolecular synthesis to 17 beta-acetamido-3-aza-A-homo-4 alpha-androsten-4-one

Cancer Invest. 1987;5(4):301-7.

Abstract

17 beta-acetamido-3-aza-homo-4 alpha-androsten-4-one has cytostatic activity against Ehrlich ascites tumor, L1210, and P388 leukemias in mice when administered intraperitoneally. The effect of the homo-aza-steroid on the incorporation of radioactive precursors to DNA and RNA of L1210 leukemia cells was investigated. It was found that treatment of cells with 12.5 micrograms/ml of the drug for 1 hour inhibited DNA synthesis by 81%. This was partly because the drug affected the radioactive thymidine pool in the cell. The inhibitory effect was found to be reversable. The incorporation of [3H]thymidine into DNA was lower when cells were incubated in the presence of S9 mix. It was also found that the same compound inhibited RNA synthesis by 67%.

MeSH terms

  • Androstenes / metabolism
  • Androstenes / pharmacology*
  • Androstenes / therapeutic use
  • Animals
  • Azasteroids / metabolism
  • Azasteroids / pharmacology*
  • Azasteroids / therapeutic use
  • Carcinoma, Ehrlich Tumor / drug therapy*
  • Carcinoma, Ehrlich Tumor / metabolism
  • DNA, Neoplasm / biosynthesis*
  • Female
  • Leukemia L1210 / drug therapy*
  • Leukemia L1210 / metabolism
  • Leukemia P388 / drug therapy*
  • Leukemia P388 / metabolism
  • Leukemia, Experimental / drug therapy*
  • Mice
  • Mice, Inbred DBA
  • Neoplasm Transplantation
  • Steroids, Heterocyclic / pharmacology*
  • Time Factors
  • Tumor Cells, Cultured

Substances

  • Androstenes
  • Azasteroids
  • DNA, Neoplasm
  • Steroids, Heterocyclic
  • 17-acetamido-3-aza-A-homo-4-androsten-4-one