Synthesis of aminoalkyl-substituted polymethoxychalcone derivatives and their antiproliferative activities against three human cancer cell lines

Two novel series of sixteen aminoalkyl-substituted polymethoxychalcone derivatives 2a―2h and 3a―3h were synthesized from 2′-hydroxy-3,4,5,4′,6′-pentamethoxy chalcone(1) through extending alkoxy side chain at the 2′-position, and introducing amine hydrogen bond receptor at the end of the side chain. The structures of all the synthesized compounds were confirmed by 1H NMR, 13C NMR and MS techniques. Furthermore, all the compounds were tested for antiproliferative activities in vitro against a panel of three human cell lines(HeLa, HCC1954 and SK-OV-3) via CCK-8 assay. The results show that all the target compounds exhibit antiproliferative activities against the three human cancer cells with IC50 values of 4.62―48.21 μmol/L, except compound 2h against SK-OV-3 cells. Most of these compounds were more active when compared to the positive control cis-Platin.