Abstract:
Two naturally occurring flavones, apigenin-5, 4'-dimethy ether(1) and lutedin-5, 3', 4'-trimethyl ether(2), were synthesized through I2/Py dehydrogenation, O-methylation and glycoside hydrolysis reaction, using naringin and hesperidin as raw materials.Based on Mannich reaction of flavones 1 or 2 with various secondary amines and formaldehyde in acidic alcohol solvent with microwave assisted, fifteen novel flavones Mannich base derivatives 1-17 were synthesized.The structures of all synthesized compounds were confirmed by 1H NMR, 13C NMR and MS techniques.Furthermore, all compounds were tested for anti-proliferative activities on human cervical carcinoma Hela cells using cell counting Kit-8(CCK-8).The results showed that compounds 1, 2, 7, 9, 10, 12 and 17 exhibited distinct anti-proliferative activities against Hela cells.Among them, compounds 10, 12 and 17 displayed higher activities with inhibitory concentration 50%(IC50) of 16.13, 29.04 and 9.14 μmol/L than the positive control cis-platin(IC50=41.25 μmol/L).