Synthesis and antitumor activity of silibinin derivatives targeting VEGFR

Totally 10 inhibitors of VEGFR based on silibinin derivatives were designed and synthesized with the modification on the hydroxyl group at C-3 and C-7 positions of silibinin through acylation, selective aminolysis, alkylation, oxidation, and dehydrogenation reactions. Their structures were confirmed by MS, ¹H NMR, and ¹³C NMR. <i>In vitro</i> activity assay showed that these compounds can inhibit cell proliferation of A549 and SGC7901 cells, especially compounds <b>I₃</b> and <b>I₈</b> showed better inhibitory activity on these tumor cells, and similar to the positive control drug lapatinib, which may be potential candidate compounds for tumor therapy.