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.

Effects of [Cu(2-MeSNic)2(MeNia)2(H2O)2]·H2O and [Cu(2-MeSNic)2(H2O)]2 on Candida albicans

“…1A). R value less than one is characteristic for biologically active substances that interfere with energy metabolism cells directly or indirectly by affecting the integrity of biological membranes (Majtán and Drobnica, 1982;Miko et al, 1991;Miko and Devínsky, 1993a;Miko and Devínsky, 1993b). 1B).…”

Benfluron Induces Cell Cycle Arrest, Apoptosis and Activation of p53 Pathway in MOLT-4 Leukemic Cells

“…The cytostatic and cytotoxic effects of BF were also proved in the studies performed in vitro. Inhibition of cell proliferation was proved in HeLa and V/79 cells (Horáková et al, 1988), Ehrlich carcinoma cells and P388 leukaemia cells (Miko et al, 1989). As well, Soucek et al (1987) showed that BF had a significant cytostatic effect on nine human leukemic cell lines in vitro.…”

“…Early studies assessed the influence of BF on the cell metabolism, proliferation and cell membrane integrity. It was established that benfluron may influence cell membrane processes, as well as synthesis of proteins and nucleic acids (Miko et al, 1989). The final cytotoxic effect of BF is concentration-dependent and differs in various cell types.…”