Primary screening and inhibition of macromolecular biosynthesis in Ehrlich ascites cells by benzo(C)fluorene derivatives.

Abstract

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.

• Authors: M Miko, J Krepelka, M Melka
• Journal: Drug metabolism and drug interactions (Drug Metabol Drug Interact) Vol. 9 Issue 1 Pg. 1-22 ( 1991) ISSN: 0792-5077 [Print] Germany
• PMID: 1893750 (Publication Type: Journal Article)

Chemical References

• DNA, Neoplasm
• Fluorenes
• Neoplasm Proteins
• RNA, Neoplasm
• benzo(c)fluorene
• Valine
• Adenine
• Tilorone
• Thymidine
• Uridine

Topics

• Adenine (metabolism)
• Animals
• Carcinoma, Ehrlich Tumor (metabolism)
• DNA, Neoplasm (biosynthesis)
• Drug Screening Assays, Antitumor
• Fluorenes (pharmacology)
• Mice
• Mice, Inbred Strains
• Neoplasm Proteins (biosynthesis)
• RNA, Neoplasm (biosynthesis)
• Thymidine (metabolism)
• Tilorone (pharmacology)
• Tumor Cells, Cultured
• Uridine (metabolism)
• Valine (metabolism)