Primary screening and inhibition of macromolecular biosynthesis in Ehrlich ascites cells by benzo(C)fluorene derivatives.
The main objective of the present investigation was to screen a series of new benzo(c)fluorene compounds for in vitro activity. It can be stated that each of the 9 newly synthesized benzo(c)fluorene derivatives was about 10 times as active as tilorone. To elucidate the biochemical mode of action, the effects of 2 new compounds (13468 and 14200) on biosynthesis of macromolecules indicated by the incorporation rate of [14C]adenine (DNA, RNA), [14C]-thymidine (DNA), [14C]uridine (RNA) and [14C]valine (protein) were studied in concentration and time dependence. Both compounds inhibited the incorporation of the 4 precursors into the TCA-insoluble fraction of Ehrlich ascites carcinoma cells.
Miko
M
M
Department of Microbiology and Biochemistry, Slovak Polytechnic University, Bratislava.
Krepelka
J
J
Melka
M
M
D000225:Adenine / Q000378:metabolism; D000818:Animals; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism*; D004273:DNA, Neoplasm / Q000096:biosynthesis; D004354:Drug Screening Assays, Antitumor; D005449:Fluorenes / Q000494:pharmacology*; D051379:Mice; D008815:Mice, Inbred Strains; D009363:Neoplasm Proteins / Q000096:biosynthesis; D012334:RNA, Neoplasm / Q000096:biosynthesis; D013936:Thymidine / Q000378:metabolism; D013994:Tilorone / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D014529:Uridine / Q000378:metabolism; D014633:Valine / Q000378:metabolism
D004273:DNA, Neoplasm; D005449:Fluorenes; D009363:Neoplasm Proteins; D012334:RNA, Neoplasm; C041513:benzo(c)fluorene; D014633:Valine; D000225:Adenine; D013994:Tilorone; D013936:Thymidine; D014529:Uridine