5 - (instead Of Pyridine) - 2 H - Pyran - 2 - Ketone Derivatives Synthesis And Antitumor Activity

2H-pyran-2-one is a unsaturated lactone structure which has six-membered ring. It is highly abundant in bacteria, microbial, plant, insect and animal systems and takes part in many different types of biological processes, such as defence against other organisms, as key biosynthetic intermediates, and as metabolites. Historically,2H-pyran-2-ones are used as precursors for the synthesis of biologically important compounds such as pheromones, solanopyrones,α-chymotrysin, elastase, coumarins and analogues.Separated by SK chemicals, natural product SK-F12 is a 5-substituted-2-pyran-2-one with an IC50 value of 0.0014 ug/mL in the inhibition of A549. Basing on the chemical structure and biological activity of SK-F12, we have designed and synthesized a series of compounds of 5-(substituted phenyl)-2H-pyran-2-ones in our previous work. Anti-tumor activity screens in vitro showed that compounds of 5-substituted-2H-pyran-2-ones have good inhibition of A549.Basing on the theory of bioisosteris, We designed a series compounds of 5-(heterocyclic substituted)-2H-pyran-2-ones, and synthesized seven compounds of 5-(substituted pyridine)-2H-pyran-2-ones and one compound of 5-(furan)-2-pyran-2-one through stille coupling reaction, which are all innovative and have not been reported yet. The structures of the compounds were identified by1H-NMR and MS.Hoping to screen out compounds which have higher activity.