Synthesis And Anticancer Activity Study On A-aminophosphonate Derivatives Containing Thieno[3,2-c]Pyridine

Thienopyridine, like quinoline and isoquinoline, is a kind of fused heterocycle compounds, which has been found widely in natural drugs. Studies indicate that many thienopyridine compounds have attracted more and more attentions since their wide range of biological activities such as anti-bacterial, anti-cancer, anti-thrombotic and phytocidal. Meanwhile, the study of a-aminophosphonate derivatives has been becoming one of the presently studying hotspots due to their excellent biological activities. They were used as fungicides, anticancers, antioxidant, enzyme inhibitors, plant virucides and herbicides in clinic. According to the pharmacological principle of stacking, twenty-one novel a-aminophosphonates containing thieno[3,2-c]pyridine were synthesized in order to obtain new compounds which possess better biological activity. All these target products have not been reported in literature, and their structures were confirmed by1H NMR、13C NMR、31P NMR、 IR、 ESI-MS and HRMS.In addition, the inhibitory effect of target compounds against EC109, HepG2and MGC803cells were determined preliminarily. Some compounds showed excellent activity and superior to the positive control drug5-fluorouracil.