Miko M, Devinsky F
Department of Microbiology, Biochemistry and Biology, Slovak Technical University, Bratislava.
Neoplasma. 1993;40(3):153-9.
A new class of nonaromatic amine oxides was synthesized and tested for cytotoxic activity in vitro. The aim of this study was to find if there is any correlation between the cytotoxic activity of the investigated 1-alkylpyrrolidine N-oxides and their structure (as a structural parameter the number of carbon atoms m in the alkyl chain was used). Maximum activity was achieved with 1-tetradecylpyrrolidine N-oxide (C14) which was chosen for further biochemical studies. Further lengthening led to decrease in activity. The drug inhibited the incorporation rate of [14C] precursors (adenine, thymidine, uridine, valine) into appropriate macromolecules of Ehrlich ascites cells, the extent of inhibition being dependent on both time and concentration of the compound in the incubation medium.
合成了一类新型的非芳香族氧化胺，并对其体外细胞毒性活性进行了测试。本研究的目的是确定所研究的1-烷基吡咯烷N-氧化物的细胞毒性活性与其结构之间是否存在任何相关性（作为结构参数，使用烷基链中碳原子的数量m）。1-十四烷基吡咯烷N-氧化物（C14）达到了最大活性，该化合物被选用于进一步的生化研究。进一步延长烷基链会导致活性降低。该药物抑制了[14C]前体（腺嘌呤、胸腺嘧啶核苷、尿苷、缬氨酸）掺入艾氏腹水癌细胞的相应大分子中，抑制程度取决于孵育培养基中化合物的时间和浓度。
