Design, Synthesis and Bioactivities of Novel 1,4-Pentadien-3-one Derivatives Containing a Substituted Pyrazolyl Moiety

In this study, in order to find novel biologically active penta-1,4-dien-3-one derivatives, a series of penta-1,4-dien-3-one compounds containing a substituted pyrazole subunit were designed and synthesized. Their structures were characterized by (1)H-NMR, (13)C-NMR and elemental analysis. The preliminary bioassays displayed that most of the title compounds showed significant antiproliferative activity against HepG2 cell lines. Especially, compounds 7a–m, o, r, s, u, w, y and z were active against HepG2 cells with IC(50) values of 0.10–5.05 μM, which were superior to that of the contrast sorafenib (IC(50) = 16.20 μM).