Response of transplantable tumors in mice and of macromolecular synthesis to 17 beta-acetamido-3-aza-A-homo-4 alpha-androsten-4-one.
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%.
Athanasiou
C
C
Laboratory of Pharmaceutical Chemistry, University of Patras, Greece.
Catsoulacos
P
P
Papageorgiou
A
A
Athanasiou
K
K
D000736:Androstenes / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D001378:Azasteroids / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy* / Q000378:metabolism; D004273:DNA, Neoplasm / Q000096:biosynthesis*; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy* / Q000378:metabolism; D007941:Leukemia P388 / Q000188:drug therapy* / Q000378:metabolism; D007942:Leukemia, Experimental / Q000188:drug therapy*; D051379:Mice; D008811:Mice, Inbred DBA; D009368:Neoplasm Transplantation; D013260:Steroids, Heterocyclic / Q000494:pharmacology*; D013997:Time Factors; D014407:Tumor Cells, Cultured
D000736:Androstenes; D001378:Azasteroids; D004273:DNA, Neoplasm; D013260:Steroids, Heterocyclic; C054024:17-acetamido-3-aza-A-homo-4-androsten-4-one