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

Abstract

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.

Keywords

Polymethoxychalcone / Aminoalkyl-substituted derivative / Antiprolifertive activity

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