The invention provides a preparation method of a class of flavone-ligustrazine series derivatives, and applications of the flavone-ligustrazine series derivatives in preparation of antitumor drugs. According to the invention, the compound has obvious inhibition activity on the growth of tumor
cell lines (HepG-2, Bel-7402, MCF-7, HT-29 and
Hela), and almost does not affect a human normal vascular endothelial
cell (HUVEC-12) line, the
antitumor activity of part of the compounds is similar to the
antitumor activity of a positive
drug cis-
platinum; the compound CH-5 has
high selectivity between tumors and between tumors and
normal cell lines, and has the strongest inhibition effect on
liver cancer (Bel-7402), wherein the IC50s of the compound to HepG-2, Bel-7402, HT-29, MCF-7 and
Hela respectively are 17.31+ / -0.47 [mu]M, 10.74+ / -1.12 [mu]M, 31.88+ / -1.96 [mu]M, 29.79+ / -2.18 [mu]M and 25.11+ / -1.80 [mu]M; and the compound CH-5 has no killing effect on HUVEC-12 cells while inhibiting
cancer cells, and shows a certain proliferation promoting activity.