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, H NMR, and C NMR. activity assay showed that these compounds can inhibit cell proliferation of A549 and SGC7901 cells, especially compounds and 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.