Emodin belongs to the anthraquinone class of compounds and is the major bioactive compound of several herb species. A library of novel emodin derivatives was synthesized and their antiproliferative activities were evaluated against HepG2, PC-3, DU-145, MCF-7, and HEK-293 cell lines. Among these derivatives, one showed a higher order of in vitro anticancer activity profile similar to the market drug epirubicin. The derivative strongly inhibited the proliferation of HepG2, PC-3, DU-145 and MCF-7 cancer cell lines with IC50 values of 3.5, 5.6, 7.5, and 4.5 μM respectively. The derivative was also capable of inducing caspase-3-mediated apoptosis in HepG2 cells by arresting the cell cycle in the S phase. Furthermore, the derivative exhibited DNA intercalating ability comparable to doxorubicin, thus making this compound a promising potential antitumor drug.
