Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains
Abstract A series of methylthiazonaphthalimides was synthesized and quantitatively evaluated as efficient DNA intercalators, antitumor agents and DNA photocleavers. A 1 showed both efficient antitumor activities against cell lines of A549 and P388 with IC 50 of 82.8 and 31 nM, respectively. A 3 was the strongest antitumor agent against A549 with the IC 50 of 20.8 nM. A 2 , the most efficient DNA intercalator, was found to be the strongest DNA photocleaver via superoxide anion. An explanation was given for the disaccord between antitumor and DNA photocleaving activities.
A study was carried out on the separation of active anthraquinone ingredient in Chinese rhubarb using High-Speed Countercurrent Chromatography with acid-base accommodationt. Trifluoroacetic acid (TFA) was used as the retaining acid and ammonia liquor as the eluent base. The solvent system was n-hexane-acetic ester-methanol-water (ratio by volume was 9 ∶1 ∶5 ∶5). The separative product was confirmed as five pure anthraquinone of Chinese rhubarb by High Performance Liquid Chromatography (HPLC).