Synthesis Of The Prenylated Chalcones And Their Anti-cancer Activities

Cancer is one of the major causes of death worldwide and chemotherapy is the primary treatment for this disease.The curative effects of most existing chemotherapy drugs are still far from satisfactory,therefore,the research and development for more effective and safe anticancer agents is particulatly important.Natural products with anticancer activity are the main source for the screening of new antitumor medicines.Chalcones,known as?,?-unsaturated ketones,a major component of the natural products.Chalcones as well as their synthetic analogues display enormous number of biological activities,such as anti-tumor,anti-inflammatory,anti-bacterial,etc.A series of prenylated chalcone were reported have significant inhibitory activity against lung cancer,liver cancer,cervical cancer,leukemia and other cancer cells,and some research indicated that the prenyl substituent on chalcone can increase the binding capacity with biofilm,and thus improve the anticancer activity of these compounds.In addition,the structure of this kind of chemicals is quite simple to synthesize,so they exhibit tremendous potential to act as antitumor agents.Based on that,we report herein the design of a series of prenylated chalcones,including two types of single prenylated chalcones,one class of double prenylated chalcones and one kind of novel double prenylated chalcones which B ring was placed by azaheterocycle,and their structures were confirmed by ESI-MS,¹H NMR and ¹³C NMR.The anti-cancer activities of those compounds were evaluated in vitro,in particular,the compound T41 showed promising bioactivities against PC3,MDA,HEL and K562 cells with inhibition rate of 83.4%,33.4%,85.4%and 88.8%at the concentration of 5μmol·L^-1,respectively.This research will provide a reference in the study of the synthetic methods and anti-cancer activity for the prenylated chalcones.