Miko M, Krepelka J, Melka M
Department of Microbiology and Biochemistry, Slovak Polytechnic University, Bratislava.
Drug Metabol Drug Interact. 1991;9(1):1-22. doi: 10.1515/dmdi.1991.9.1.1.
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.
本研究的主要目的是筛选一系列新型苯并(c)芴化合物的体外活性。可以说，新合成的9种苯并(c)芴衍生物中的每一种的活性约为泰洛龙的10倍。为阐明其生化作用模式，研究了2种新化合物（13468和14200）对[14C]腺嘌呤（DNA、RNA）、[14C]胸腺嘧啶核苷（DNA）、[14C]尿苷（RNA）和[14C]缬氨酸（蛋白质）掺入率所指示的大分子生物合成的影响，研究了其浓度和时间依赖性。两种化合物均抑制4种前体掺入艾氏腹水癌细胞的三氯乙酸不溶性部分。
